| Assay ID | Title | Year | Journal | Article |
|---|
| AID1250656 | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1566043 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID1250640 | Inhibition of recombinant human HDAC1 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID570247 | Activation of Runx2 activity in mouse C2C12 cells at 50 nM after 24 hrs by luciferase reporter gene assay relative to control | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID775178 | Inhibition of HDAC3 (unknown origin) using MAZ1600 and MAZ1675 as substrate assessed as fluorogenic release of 7-amino-4-methylcoumarin from substrate by optimized homogenous assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
| Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. |
| AID1250644 | Inhibition of recombinant human HDAC4 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID725670 | Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate additio | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
| AID777256 | Cytotoxicity against human H466 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777257 | Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1566036 | Selectivity index, ratio of IC50 for recombinant human HDAC6 to IC50 for recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID492802 | Inhibition of human recombinant HDAC4 at 5 uM after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1189017 | In vivo inhibition of HDAC in tumor of human HCT116 cells xenografted nu/nu mouse assessed as increase in histone hyperacetylation at 50 mg/kg, po after 4 to 12 hrs by immunoblotting method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID1250658 | Selectivity ratio of GI50 for human DU145 cells to GI50 for human HLF cells | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1225369 | Cytotoxicity against human HT-29 cells assessed as cell viability at 4 nM incubated for 48 hrs in presence of 0.32 nM dolastatin 10 by MTT assay | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3
| Targeted natural products discovery from marine cyanobacteria using combined phylogenetic and mass spectrometric evaluation. |
| AID1189000 | Drug metabolism in human HCT116 cells protein lysate solution assessed as largazole thiol formation at 25 ug/mL after 30 mins by HPLC-MS method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID777246 | Cell cycle arrest in human A549 cells assessed as accumulation at G2 phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 3.7%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1234525 | Inhibition of recombinant full-length HDAC6 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID630806 | Inhibition of recombinant HDAC1 at 1 uM after 1 hr by fluorimetric assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID1323321 | Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7
| Caldoramide, a Modified Pentapeptide from the Marine Cyanobacterium Caldora penicillata. |
| AID777250 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 48%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID492809 | Effect on differentiation of human NB4 cells assessed as induction of CD11c expression at 5 uM after 48 hrs by propidium iodide staining-base FACS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1163398 | Inhibition of human HDAC1 (unknown origin) at 0.01 to 5 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID1234524 | Inhibition of recombinant full-length HDAC3 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID1566045 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID777221 | Inhibition of HDAC-1 in human NCI-H460 cells assessed as accumulation of hyperacetylated H3 at 0.1 uM after 6 to 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1431818 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID492806 | Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 5 uM after 24 hrs by FACS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1466448 | Inhibition of class 1 HDAC in human HCT116 cells assessed as hyperacetylation of histone H3 (Lys9/14) measured at 8 hrs post treatment by immunoblot analysis | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and biological evaluation of largazole zinc-binding group analogs. |
| AID1323323 | Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction of cell viability measured after 48 hrs by ATPlite 1step luminescence assay relative to parental HCT116 cells | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7
| Caldoramide, a Modified Pentapeptide from the Marine Cyanobacterium Caldora penicillata. |
| AID1446910 | Inhibition of Schistosoma mansoni KDAC8 at 30 uM using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy. |
| AID570499 | Osteogenic activity in mouse C2C12 cells assessed as increase of Runx2 mRNA expression at 50 nM after 6 days by RT-PCR analysis relative to control | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1655610 | Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| AID777214 | Inhibition of E2F1 in human A549 cells assessed as downregulation of DHFR gene expression at 0.1 uM after 6 to 36 hrs by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777238 | Induction of apoptosis in human A549 cells assessed as downregulation of pro-caspase-9 protein expression at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1189009 | In vivo inhibition of HDAC in tumor of human HCT116 cells xenografted nu/nu mouse assessed as increase in histone hyperacetylation at 10 mg/kg, ip after 4 to 24 hrs by immunoblotting method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID777199 | Downregulation of p21 protein expression in human A549 cells at 0.1 uM after 4 hrs by Western blotting analysis in presence of protein synthesis inhibitor cycloheximide | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1686620 | Growth inhibition of human NCI-60 cells at 10 uM | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID1566038 | Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID1686642 | Selectivity index, ratio of IC50 for recombinant HDAC6 (unknown origin) to IC50 for recombinant HDAC3 (unknown origin) | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID630871 | Inhibition of HDAC6 in human HCT116 cells assessed as increase in alpha tubulin acetylation at 0.01 to 1 uM after 24 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID1189016 | Drug metabolism in tumor of human HCT116 cells xenografted nu/nu mouse assessed as time for maximum largazole thiol level at 50 mg/kg, ip by HPLC-MS method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID1250650 | Inhibition of recombinant human HDAC11 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID725667 | Inhibition of C-terminal His-tagged human recombinant HDAC9 (amino acids 604- 1066) expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured afte | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
| AID630807 | Inhibition of HDAC1 from human HeLa nuclear extract after 1 hr by fluorimetric assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID1280300 | Inhibition of full length human recombinant KDAC6 using fluorophore-conjugated substrate measured as fluorigenic release of 7-amino-4-methylcoumarin by microtiter plate reader analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
| AID1431811 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1163401 | Inhibition of human HDAC1 (unknown origin) at 0.1 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID777230 | Effect on cyclin D1 protein expression in human A549 cells at 0.1 uM after 6 to 36 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1234527 | Cytotoxicity against human NMC-797 cells assessed as cell viability after 48 hrs by luminescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID492804 | Inhibition of human recombinant HDAC4 after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID777231 | Upregulation of p27 protein expression in human A549 cells at 0.1 uM after 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777241 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at S phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 31.6%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1234528 | Cytotoxicity against human NMC-10326 cells assessed as cell viability after 48 hrs by luminescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID777228 | Effect on CDK2 protein expression in human A549 cells at 0.1 uM after 6 to 36 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777200 | Induction of E2F1 ubiquitination in human A549 cells at 0.1 uM after 8 hrs by immunoprecipitation and Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777201 | Induction of E2F1 degradation in human A549 cells at 0.1 uM after 12 hrs by Western blotting analysis in presence of proteasome inhibitor MG-132 | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID570507 | Osteogenic activity in mouse assessed as induction of woven bone formation at 50 uM administered with collagen sponges in calvarial bone after 3 weeks | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1250653 | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1280299 | Inhibition of full length human recombinant KDAC3 using fluorophore-conjugated substrate measured as fluorigenic release of 7-amino-4-methylcoumarin by microtiter plate reader analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
| AID603218 | Inhibition of HDAC in human HeLa cell extracts assessed as conversion of dithiothreitol to dithiol after 1 hr by Flour-de-Lys assay | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID1163404 | Inhibition of human HDAC in human HCT116 cells assessed as global histone H3 lysine-9 acetylation levels at 0.01 to 1 uM after 24 hrs by Western blotting method | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID570502 | Osteogenic activity in mouse C2C12 cells assessed as increase of BMP6 mRNA expression at up to 50 nM after 6 days by RT-PCR analysis | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1250645 | Inhibition of recombinant human HDAC5 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID630869 | Inhibition of HDAC1 in human HCT116 cells assessed as increase in histone H3 acetylation at 100 nM after 24 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID630809 | Inhibition of recombinant HDAC6 at 1 uM after 1 hr by fluorimetric assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID1686619 | Growth inhibition of human HCT-116 cells incubated for 96 hrs by MTS assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID1250654 | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID777209 | Induction of E2F1 degradation in human NCI-H1975 cells at 0.1 uM after 12 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777258 | Cytotoxicity against human 95-D cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777262 | Cytotoxicity against human GLC82 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1655608 | Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | | | |
| AID777264 | Cytotoxicity against human NCI-H1975 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1686641 | Selectivity index, ratio of IC50 for recombinant HDAC6 (unknown origin) to IC50 for recombinant HDAC2 (unknown origin) | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID777236 | Induction of apoptosis in human A549 cells assessed as effect on caspase-8 protein expression at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777226 | Downregulation of p21 protein expression in human A549 cells at 0.1 uM after 1 hr by Western blotting analysis in presence of protein synthesis inhibitor cycloheximide | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1280301 | Inhibition of full length human recombinant KDAC8 using fluorophore-conjugated substrate measured as fluorigenic release of 7-amino-4-methylcoumarin by microtiter plate reader analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
| AID1431812 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1566044 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID1234522 | Inhibition of recombinant full-length HDAC1 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID603217 | Inhibition of HDAC in human MCF7 cells assessed as accumulation of H4K8(ac) at 100 nM by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID1234526 | Inhibition of recombinant full-length HDAC8 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID1686637 | Inhibition of recombinant HDAC2 (unknown origin)incubated for 15 mins before substrate addition and measured after 30 to 45 mins by HDAC-Glo substrate | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID1250648 | Inhibition of recombinant human HDAC6 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1189012 | In vivo inhibition of HDAC in tumor of human HCT116 cells xenografted nu/nu mouse assessed as increase in histone hyperacetylation at 50 mg/kg, ip after 4 to 24 hrs by immunoblotting method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID777225 | Upregulation of p21 protein expression in human A549 cells at 0.1 uM after 6 hrs by Western blotting analysis in presence of Hsp90 inhibitor 17-AAG | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777259 | Cytotoxicity against human L78 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID670506 | Inhibition of recombinant fluorescein-tagged E1 assessed as inhibition of ubiquitin-E1 adduct formation incubated for 15 mins prior to ATP addition measured after 5 mins by SDS PAGE analysis | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Hyrtioreticulins A-E, indole alkaloids inhibiting the ubiquitin-activating enzyme, from the marine sponge Hyrtios reticulatus. |
| AID1566041 | Inhibition of full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 240 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID727135 | Inhibition of N-terminal GST-tagged human UAE-catalyzed UAE-Ub thioester intermediate formation expressed in HI5 insect cells after 15 mins by SDS-PAGE analysis | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Exploring a new frontier in cancer treatment: targeting the ubiquitin and ubiquitin-like activating enzymes. |
| AID1323324 | Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay relative to parental HCT116 cells | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7
| Caldoramide, a Modified Pentapeptide from the Marine Cyanobacterium Caldora penicillata. |
| AID1566040 | Inhibition of recombinant human HDAC6 using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID777244 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at S phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 31.6%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1163402 | Inhibition of human HDAC6 (unknown origin) at 1 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID1686622 | Inhibition of HDAC in human HCT-116 cells assessed increase in global histone H3 lysine 9 acetylation at 10 nM incubated for 24 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID492803 | Inhibition of human recombinant HDAC1 after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID492805 | Cell cycle arrest in human NB4 cells assessed as increase in accumulation at pre-G1 phase at 1 uM after 24 hrs by FACS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1156058 | Inhibition of recombinant human HDAC6 using Boc-Lys(epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay | 2014 | ACS medicinal chemistry letters, Jun-12, Volume: 5, Issue:6
| Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors. |
| AID727134 | Inhibition of human SAE by fluorescence assay | 2013 | Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
| Exploring a new frontier in cancer treatment: targeting the ubiquitin and ubiquitin-like activating enzymes. |
| AID777251 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 48.3%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID603213 | Growth inhibition of human MCF7 cells | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID777240 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G2 phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 9.5%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1323322 | Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7
| Caldoramide, a Modified Pentapeptide from the Marine Cyanobacterium Caldora penicillata. |
| AID775177 | Inhibition of HDAC6 (unknown origin) using MAZ1600 and MAZ1675 as substrate assessed as fluorogenic release of 7-amino-4-methylcoumarin from substrate by optimized homogenous assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
| Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. |
| AID777216 | Dephosphorylation of Rb in human A549 cells assessed as increase in Rb-E2F1 interaction at 0.1 uM after 8 hrs by immunoprecipitation and Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1431821 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID570244 | Inhibition of HDAC in mouse C2C12 cells assessed as increase of acetylated histone level after 24 hrs by Western blotting | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1250643 | Inhibition of recombinant human HDAC8 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1566037 | Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence b | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID1250655 | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1847749 | Inhibition of HDAC4 (unknown origin) | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
| AID777213 | Inhibition of E2F1 in human A549 cells assessed as downregulation of PCNA gene expression at 0.1 uM after 6 to 36 hrs by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1250649 | Inhibition of recombinant human HDAC10 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID777211 | Downregulation of E2F1 protein expression in human A549 cells at 0.1 uM by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1156054 | Inhibition of recombinant human HDAC1 using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2014 | ACS medicinal chemistry letters, Jun-12, Volume: 5, Issue:6
| Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors. |
| AID777202 | Induction of E2F1 degradation in human A549 cells at 0.1 uM after 12 hrs by Western blotting analysis in presence of proteasome inhibitor bortezomib | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1566039 | Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed b | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID777204 | Downregulation of E2F1 in human A549 cell nucleus at 0.1 uM after 6 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID570246 | Induction of osteoblast differentiation in mouse C2C12 cells assessed as increase of osteopontin expression up to 100 nM after 6 days | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID777203 | Downregulation of E2F1 in human A549 cell cytoplasm at 0.1 uM after 6 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777234 | Induction of apoptosis in human A549 cells assessed as decrease in pro-caspase-3 level at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1466444 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and biological evaluation of largazole zinc-binding group analogs. |
| AID1686639 | Inhibition of recombinant HDAC6 (unknown origin)incubated for 15 mins before substrate addition and measured after 30 to 45 mins by HDAC-Glo substrate | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID1323320 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay | 2016 | Journal of natural products, 07-22, Volume: 79, Issue:7
| Caldoramide, a Modified Pentapeptide from the Marine Cyanobacterium Caldora penicillata. |
| AID1686638 | Inhibition of recombinant HDAC3 (unknown origin)incubated for 15 mins before substrate addition and measured after 30 to 45 mins by HDAC-Glo substrate | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID777219 | Inhibition of HDAC-1 in human 16HBE cells assessed as accumulation of hyperacetylated H3 at 0.1 uM after 6 to 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1250647 | Inhibition of recombinant human HDAC9 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID630804 | Growth inhibition of human HCT116 cells after 96 hrs by MTS assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID1431814 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID775180 | Inhibition of HDAC1 (unknown origin) using MAZ1600 and MAZ1675 as substrate assessed as fluorogenic release of 7-amino-4-methylcoumarin from substrate by optimized homogenous assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
| Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. |
| AID777252 | Cytotoxicity against human NCI-H460 cells assessed as inhibition of colony formation pretreated for 24 hrs followed by seeding measured after 10 days by clonogenic assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777212 | Induction of HDAC1-mediated E2F1 deacetylation in human A549 cells at 0.1 uM after 8 hrs by immunoprecipitation and Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1156056 | Inhibition of recombinant human HDAC3 using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay | 2014 | ACS medicinal chemistry letters, Jun-12, Volume: 5, Issue:6
| Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors. |
| AID492812 | Induction of p21WAF1/CIP1 expression in human NB4 cells at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID777255 | Growth inhibition of human A549 cells at 0.1 uM after 24 to 48 hrs by trypan blue exclusion assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1655614 | Antiproliferative activity against human IMR32 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | | | |
| AID777239 | Induction of apoptosis in human A549 cells at 0.3 to 1 uM after 48 hrs by Annexin V and propidium iodide staining-based flow cytometric analysis relative to control | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1655613 | Antiproliferative activity against human Caco2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| AID1431819 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID570508 | Osteogenic activity in rabbit calvarial bone fracture healing model assessed as bone formation at 100 to 200 nM after 4 weeks | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1655611 | Antiproliferative activity against human Caco2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | | | |
| AID630868 | Inhibition of HDAC1 in human HCT116 cells assessed as increase in histone H3 acetylation at 10 nM after 24 hrs by Western blot analysis | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID777248 | Cell cycle arrest in human A549 cells assessed as accumulation at G1 phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 48.3%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID492808 | Effect on differentiation of human NB4 cells assessed as induction of CD11c expression at 5 uM after 24 hrs by propidium iodide staining-base FACS analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1655615 | Antiproliferative activity against human IMR32 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | | | |
| AID1188998 | Inhibition of HDAC in human HCT116 cells assessed as increase in histone H3 (Lys9/14) hyperacetylation after 8 to 24 hrs by immunoblotting method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID570245 | Induction of osteoblast differentiation in mouse C2C12 cells assessed as increase of alkaline phosphatase expression after 6 days | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID630808 | Inhibition of HDAC6 from human HeLa nuclear extract after 1 hr by fluorimetric assay | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: synthesis and biological evaluation. |
| AID777217 | Dephosphorylation of Rb in human A549 cells at 0.1 uM after 6 to 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1431816 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID777253 | Growth inhibition of human NCI-H460 cells at 0.1 uM after 24 to 48 hrs by trypan blue exclusion assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777205 | Induction of E2F1 translocation from nucleus to cytoplasm in human A549 cells at 0.1 uM after 12 to 24 hrs by DAPI staining-based immunofluorescence analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777263 | Cytotoxicity against human A549 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777235 | Induction of apoptosis in human A549 cells assessed as increase in cleaved caspase-3 level at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1163400 | Inhibition of human HDAC1 (unknown origin) at 1 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID1466449 | Inhibition of class 1 HDAC in human MDA-MB-231 cells assessed as hyperacetylation of histone H3 (Lys9/14) measured at 8 hrs post treatment by immunoblot analysis | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and biological evaluation of largazole zinc-binding group analogs. |
| AID777229 | Effect on CDK4 protein expression in human A549 cells at 0.1 uM after 6 to 36 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID603215 | Inhibition of HDAC in human SKBr3 cells assessed as accumulation of H4K8(ac) at 100 nM by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID777243 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G2 phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 9.5%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777247 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 48%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777207 | Induction of E2F1 degradation in human 95-D cells at 0.1 uM after 12 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1686640 | Selectivity index, ratio of IC50 for recombinant HDAC6 (unknown origin) to IC50 for recombinant HDAC1 (unknown origin) | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID570503 | Osteogenic activity in mouse C2C12 cells assessed as increase of BMP7 mRNA expression at up to 50 nM after 6 days by RT-PCR analysis | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1655616 | Antiproliferative activity against human IMR32 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | | | |
| AID725669 | Inhibition of C-terminal His-tagged full length human recombinant HDAC2 expressed in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured after 60 mins by | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
| AID1234523 | Inhibition of recombinant full-length HDAC2 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole. |
| AID570506 | Osteogenic activity in mouse assessed as induction of woven bone formation at 10 uM administered with collagen sponges in calvarial bone after 3 weeks | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID777249 | Cell cycle arrest in human A549 cells assessed as accumulation at G2 phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 3.7%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777254 | Cytotoxicity against human A549 cells assessed as inhibition of colony formation pretreated for 24 hrs followed by seeding measured after 10 days by clonogenic assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1446915 | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
| Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy. |
| AID1655612 | Antiproliferative activity against human Caco2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | | | |
| AID777237 | Induction of apoptosis in human A549 cells assessed as increase in cleaved caspase-9 level at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1189018 | Drug metabolism in tumor of human HCT116 cells xenografted nu/nu mouse assessed largazole thiol formation at 10 mg/kg, po by HPLC-MS method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID1431815 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID570242 | Cytotoxicity against mouse C2C12 cells up to 100 uM after 3 days | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1250646 | Inhibition of recombinant human HDAC7 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID777215 | Dephosphorylation of Rb in human A549 cells assessed as increase in E2F1-HDAC1 interaction at 0.1 uM after 8 hrs by immunoprecipitation and Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1163403 | Inhibition of human HDAC6 (unknown origin) at 5 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID777261 | Cytotoxicity against human NCI-H460 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID492801 | Inhibition of human recombinant HDAC1 at 5 uM after 15 mins by fluorimetric assay | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID777220 | Inhibition of HDAC-1 in human NCI-H1975 cells assessed as accumulation of hyperacetylated H3 at 0.1 uM after 6 to 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID570505 | Osteogenic activity in mouse C2C12 cells assessed as inhibition of multinucleated osteoclasts formation after 6 days | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1250641 | Inhibition of recombinant human HDAC2 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID570243 | Inhibition of HDAC in mouse C2C12 cells at 5 to 100 nM after 24 hrs by fluorescence assay | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID1655609 | Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | | | |
| AID1225366 | Cytotoxicity against human HT-29 cells assessed as cell viability at 4 nM incubated for 48 hrs by MTT assay | 2015 | Journal of natural products, Mar-27, Volume: 78, Issue:3
| Targeted natural products discovery from marine cyanobacteria using combined phylogenetic and mass spectrometric evaluation. |
| AID777245 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G1 phase at 0.06 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 58.9%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1431820 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID725666 | Selectivity ratio of IC50 for C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 to IC50 for C-terminal His-tagged human recombinant HDAC9 (amino acids 604- 1066) by fluorescence analysis | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
| AID777223 | Inhibition of HDAC-1 in human A549 cells assessed as hyperacetylation of histone H3 at 0.01 to 1 uM after 4 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1686636 | Inhibition of recombinant HDAC1 (unknown origin) incubated for 15 mins before substrate addition and measured after 30 to 45 mins by HDAC-Glo substrate | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue. |
| AID1189015 | Drug metabolism in tumor of human HCT116 cells xenografted nu/nu mouse assessed as time for maximum largazole thiol level at 10 mg/kg, ip by HPLC-MS method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID1163399 | Inhibition of human HDAC6 (unknown origin) at 0.01 to 5 uM using Fluor de Lys substrate fluorimetric assay | 2014 | European journal of medicinal chemistry, Oct-30, Volume: 86 | Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups. |
| AID1847745 | Inhibition of HDAC1 (unknown origin) | 2021 | Bioorganic & medicinal chemistry, 12-15, Volume: 52 | From natural products to HDAC inhibitors: An overview of drug discovery and design strategy. |
| AID1250642 | Inhibition of recombinant human HDAC3 after 60 mins by fluorescence assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID777222 | Inhibition of HDAC-1 in human A549 cells assessed as accumulation of hyperacetylated H3 at 0.1 uM after 6 to 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777224 | Inhibition of HDAC-1 in human A549 cells assessed as recruitment of p21 promoter to acetyl H3 at 0.1 uM by chromatin immunoprecipitation assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID570501 | Osteogenic activity in mouse C2C12 cells assessed as increase of BMP4 mRNA expression at up to 50 nM after 6 days by RT-PCR analysis | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID777233 | Induction of apoptosis in human A549 cells assessed as increase in PARP cleavage at 0.1 uM after 48 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777208 | Induction of E2F1 degradation in human L78 cells at 0.1 uM after 12 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1280298 | Inhibition of full length human recombinant KDAC1 using fluorophore-conjugated substrate measured as fluorigenic release of 7-amino-4-methylcoumarin by microtiter plate reader analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4
| Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors. |
| AID777260 | Cytotoxicity against human SPCA1 cells after 48 hrs by CCK-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1466445 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
| Synthesis and biological evaluation of largazole zinc-binding group analogs. |
| AID777206 | Induction of E2F1 degradation in human 16HBE cells at 0.1 uM after 12 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID725668 | Inhibition of C-terminal His-tagged full length human recombinant HDAC3 co-expressed with NcoR2 in baculovirus expression system using fluorogenic acetylated peptide as substrate preincubated with enzyme for 10 mins prior to substrate addition measured af | 2013 | ACS medicinal chemistry letters, Jan-10, Volume: 4, Issue:1
| Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry. |
| AID1189011 | In vivo inhibition of HDAC in tumor of human HCT116 cells xenografted nu/nu mouse assessed as increase in histone hyperacetylation at 50 mg/kg, ip after 4 hrs by immunoblotting method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID1250657 | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay | 2015 | Journal of medicinal chemistry, Oct-08, Volume: 58, Issue:19
| Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities. |
| AID1431822 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID777232 | Upregulation of p21 protein expression in human A549 cells at 0.1 uM after 6 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID775179 | Inhibition of HDAC2 (unknown origin) using MAZ1600 and MAZ1675 as substrate assessed as fluorogenic release of 7-amino-4-methylcoumarin from substrate by optimized homogenous assay | 2013 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
| Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs. |
| AID570500 | Osteogenic activity in mouse C2C12 cells assessed as increase of BMP2 mRNA expression at up to 50 nM after 6 days by RT-PCR analysis | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID570504 | Osteogenic activity in mouse C2C12 cells assessed as increase of BMP9 mRNA expression at up to 50 nM after 6 days by RT-PCR analysis | 2011 | ACS medicinal chemistry letters, Mar-10, Volume: 2, Issue:3
| In Vitro and In Vivo Osteogenic Activity of Largazole. |
| AID777242 | Cell cycle arrest in human NCI-H460 cells assessed as accumulation at G1 phase at 0.1 uM after 24 hrs by propidium iodide staining-based flow cytometric analysis (Rvb = 58.9%) | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID603216 | Inhibition of HDAC in human MDA-MB-231 cells assessed as accumulation of H4K8(ac) at 100 nM by Western blotting | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID777210 | Downregulation of E2F1 protein expression in human A549 cells after 12 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID603214 | Half life in mouse liver homogenates at 100 uM by UPLC/MS analysis | 2011 | Bioorganic & medicinal chemistry, Jun-15, Volume: 19, Issue:12
| Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability. |
| AID1431813 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID492813 | Inhibition of HDAC in human NB4 cells assessed as increase in histone H3 acetylation at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID1566046 | Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | A fluorine scan on the Zn |
| AID1189006 | Drug metabolism in mouse serum assessed as largazole thiol formation after 0.25 to 1440 mins by HPLC-MS method | 2014 | ACS medicinal chemistry letters, Aug-14, Volume: 5, Issue:8
| Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties. |
| AID777218 | Inhibition of HDAC-1 in human A549 cells assessed as induction of p21-CDK2 interaction at 0.1 uM after 4 to 8 hrs by immunoprecipitation and Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID492811 | Inhibition of HDAC in human NB4 cells assessed as increase in acetylate tubulin level at 5 uM after 24 hrs by Western blot analysis | 2010 | Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
| Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. |
| AID777265 | Induction of E2F1 degradation in human NCI-H460 cells at 0.1 uM after 12 to 24 hrs by Western blotting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID777227 | Upregulation of p21 mRNA expression in human A549 cells at 0.1 uM after 12 hrs by RT-PCR analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells. |
| AID1431817 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |