Page last updated: 2024-11-13
debio 0932
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
CUDC 305: an Hsp90 inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 44156921 |
| CHEMBL ID | 2419346 |
| SCHEMBL ID | 2995626 |
| MeSH ID | M000607537 |
Synonyms (41)
| Synonym |
|---|
| cudc305 (hsp90 inhibitor) |
| debio 0932 |
| cudc-305 |
| hsp90 inhibitor debio 0932 |
| debio-0932 |
| cudc-305,debio 0932 |
| 1061318-81-7 |
| chembl2419346 , |
| bdbm50439622 |
| SCHEMBL2995626 |
| 2-{[6-(dimethylamino)-2h-1,3-benzodioxol-5-yl]sulfanyl}-1-{2-[(2,2-dimethylpropyl)amino]ethyl}-1h-imidazo[4,5-c]pyridin-4-amine |
| DTXSID10657665 |
| HY-13469 |
| CS-5630 |
| cudc 305 |
| NCGC00387824-03 |
| cudc-305(debio 0932) |
| RVJIQAYFTOPTKK-UHFFFAOYSA-N , |
| 2-(6-(dimethylamino)benzo[d][1,3]dioxol-5-ylthio)-1-(2-(neopentylamino) ethyl)-1h-imidazo[4,5-c]pyridin-4-amine |
| unii-0v278okn9g |
| 0v278okn9g , |
| 1h-imidazo[4,5-c]pyridine-1-ethanamine, 4-amino-2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]thio]-n-(2,2-dimethylpropyl)- |
| 2-((6-(dimethylamino)benzo[d][1,3]dioxol-5-yl)thio)-1-(2-(neopentylamino)ethyl)-1h-imidazo[4,5-c]pyridin-4-amine |
| AKOS032944948 |
| 2-[[6-(dimethylamino)-1,3-benzodioxol-5-yl]sulfanyl]-1-[2-(2,2-dimethylpropylamino)ethyl]imidazo[4,5-c]pyridin-4-amine |
| debio-0932 (cudc305) |
| cudc-305, debio 0932 |
| EX-A1555 |
| AS-17028 |
| BCP27980 |
| debio0932; debio-0932; cudc305; cudc-305; cudc 305 |
| SB17222 |
| 2-((6-(dimethylamino)benzo(d)(1,3)dioxol-5-yl)thio)-1-(2-(neopentylamino)ethyl)-1h-imidazo(4,5-c)pyridin-4-amine |
| 1h-imidazo(4,5-c)pyridine-1-ethanamine, 4-amino-2-((6-(dimethylamino)-1,3-benzodioxol-5-yl)thio)-n-(2,2-dimethylpropyl)- |
| EOR , |
| debio 0932 ,cudc-305 |
| F85396 |
| 2-(6-(dimethylamino)benoz[d][1,3]dioxol-5-yl-thio)-1-(2-neopentylamino)ethyl)-1h-imidazo[4,5-c]pyridin-4-amine |
| nsc-761194 |
| nsc761194 |
| AC-35511 |
Research Excerpts
Overview
Debio 0932 is a novel oral heat shock protein 90 (Hsp90) inhibitor developed for anti-cancer therapy.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Debio 0932 is a novel oral heat shock protein 90 (Hsp90) inhibitor developed for anti-cancer therapy. " | ( Debio 0932, a new oral Hsp90 inhibitor, alleviates psoriasis in a xenograft transplantation model. Dam, TN; Gavillet, B; Rosada, C; Stenderup, K; Vuagniaux, G, 2014) | 3.29 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " CUDC-305 exhibits high oral bioavailability (96." | ( CUDC-305, a novel synthetic HSP90 inhibitor with unique pharmacologic properties for cancer therapy. Atoyan, R; Bao, R; Cai, X; DellaRocca, S; Forrester, J; Lai, CJ; Qian, C; Qu, H; Samson, M; Tao, X; Wang, D; Wang, J; Xu, GX; Yin, L; Zhai, HX; Zifcak, B, 2009) | 0.35 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (12)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 0.5868 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.9522 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 1.3878 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.7908 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Heat shock protein HSP 90-alpha | Homo sapiens (human) | IC50 (µMol) | 0.0330 | 0.0004 | 0.6950 | 10.0000 | AID767754 |
| Heat shock protein HSP 90-beta | Homo sapiens (human) | IC50 (µMol) | 0.0380 | 0.0010 | 0.6836 | 10.0000 | AID767753 |
| Endoplasmin | Canis lupus familiaris (dog) | IC50 (µMol) | 0.1900 | 0.0100 | 0.1482 | 0.5780 | AID767752 |
| Heat shock protein 75 kDa, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 1.5860 | 0.0377 | 0.4951 | 1.5860 | AID767751 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (102)
Molecular Functions (57)
Ceullar Components (50)
Bioassays (24)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1372042 | Inhibition of recombinant Caulobacter vibrioides N-terminal His6-tagged DHp-catalytic domain DivJ (188 to 585 residues) autophosphorylation expressed in Escherichia coli BL21(DE3) at 500 uM preincubated for 10 mins followed by [gamma-32P]-ATP addition aft | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372054 | Antibacterial activity against Caulobacter crescentus NA1000 after 24 hrs by broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372052 | Antibacterial activity against Escherichia coli DC2 after 24 hrs by broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372068 | Inhibition of recombinant Caulobacter vibrioides N-terminal His6-tagged DHp-catalytic domain DivJ (188 to 585 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins followed by [gamma-32P]-ATP addition after 15 mins by phosphotransfer | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372053 | Antibacterial activity against Bacillus subtilis YB886 after 24 hrs by broth dilution method | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372049 | Hemolytic activity against sheep RBC at 0.5 mM after 30 mins relative to control | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372066 | Inhibition of recombinant Caulobacter vibrioides cell cycle histidine kinase CckA deltaTM mutant DHp domain (70 to 691 residues) expressed in Escherichia coli at 250 uM in presence of varying levels of ATP measured every 60 secs for 2 hrs by PK/LDH enzyme | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID767752 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from dog Grp94 after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID1604458 | Antiproliferative activity against human MV4-11 cells after 120 hrs by TopCount scintillation analysis | 2020 | Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5 | Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions. |
| AID767753 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant HSP90beta (unknown origin) after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID767754 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID1372041 | Inhibition of recombinant Salmonella typhimurium N-terminal His6-SUMO-tagged DHp-catalytic domain PhoQ (257 to 487 residues) autophosphorylation expressed in Escherichia coli BL21(DE3) at 500 uM preincubated for 10 mins followed by [gamma-32P]-ATP additio | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372038 | Inhibition of recombinant Salmonella typhimurium N-terminal His6-SUMO-tagged DHp-catalytic domain PhoQ (257 to 487 residues) autophosphorylation expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins followed by [gamma-32P]-ATP addition after 3 | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID767751 | Displacement of 5-(3-(3-(6-amino-8-(6-iodobenzo[d][1,3]dioxol-5-ylthio)-9H-purin-9-yl)propyl)thioureido)-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid from recombinant human Trap-1 after 24 hrs by fluorescence polarization assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series. |
| AID1372065 | Inhibition of recombinant Caulobacter vibrioides cell cycle histidine kinase CckA deltaTM mutant DHp domain (70 to 691 residues) expressed in Escherichia coli in presence of varying levels of ATP measured every 60 secs for 2 hrs by PK/LDH enzyme coupled a | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| AID1372064 | Binding affinity to recombinant Caulobacter vibrioides cell cycle histidine kinase CckA delta 3 mutant DHp domain (190 to 562 residues) expressed in Escherichia coli assessed as change in metlting temperature at 30 uM after 2 mins by SYPRO orange dye base | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23 | Repurposing Hsp90 inhibitors as antibiotics targeting histidine kinases. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (15)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (13.33) | 29.6817 |
| 2010's | 7 (46.67) | 24.3611 |
| 2020's | 6 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 20.10
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.10) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (6.67%) | 5.53% |
| Reviews | 1 (6.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 13 (86.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||