knk 437 profile

KNK 437: inhibits thermotolerance acquisition and heat shock protein induction in colon carcinoma cells; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9859662
CHEMBL ID	1240927
MeSH ID	M0365038

Synonym
n-formyl-3,4-methylenedioxy-benzylidine-gamma-butyrolactam
knk-437
knk 437
CHEMBL1240927
S7750
hha56yk8lu ,
unii-hha56yk8lu
(z)-3-(benzo[d][1,3]dioxol-5-ylmethylene)-2-oxopyrrolidine-1-carbaldehyde
CCG-266914
AKOS037515497

Excerpt	Reference	Relevance
"We investigated whether the attenuation of chronic thermotolerance by KNK437, a heat shock protein inhibitor, can modify the effect of thermal radiosensitization in mild temperature hyperthermia (MTH) combined with low dose-rate irradiation (LDRI)."	( Attenuation of chronic thermotolerance by KNK437, a benzylidene lactam compound, enhances thermal radiosensitization in mild temperature hyperthermia combined with low dose-rate irradiation. Akimoto, T; Fukushima, M; Hasegawa, M; Ishikawa, H; Kitamoto, Y; Kiyohara, H; Nakano, T; Nonaka, T; Saitoh, J; Sakurai, H; Shioya, M, 2005)	0.33

Bioassays (71)

Assay ID	Title	Year	Journal	Article
AID506920	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of PARP cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506902	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as disruption of protein-Apaf-1 complex at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506949	Inhibition of HSP70-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of PARP cleavage after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506877	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as subG1 accumulation at 5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506882	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-N417 cells assessed as subG1 accumulation at 15 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242164	Inhibition of HSF1 in human ASB145 cells assessed as potentiation of 17-DMAG-induced reduction in cell proliferation at 20 uM relative to 17-DMAG alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506916	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-9 cleavage at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506898	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of Akt degradation at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506903	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of Akt degradation at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506918	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-3 cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506904	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as reduction in BAD phosphorylation at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506889	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of cell death at 10 uM after 72 hrs by propidium iodide staining-based flow cytometry in presence of broad-spectrum caspase inhibitor Boc-D-FMK	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506907	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of cell growth arrest at 20 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506900	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of Akt degradation at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506883	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-N417 cells assessed as subG1 accumulation at 25 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506944	Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as increase in caspase-3 activity after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506946	Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of PARP cleavage after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506917	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of PARP cleavage at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506910	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of cell growth arrest at 100 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506931	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of caspase-9 cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506930	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of caspase-3 cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506897	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as increased association between caspae-3 and Apaf-1 at 20 uM after 1 hr by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506950	Inhibition of HSP70-mediated antiapoptotic activity in human NCI-H526 cells assessed as release of Apaf-1 from chaperon complex after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506947	Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as release of Apaf-1 from chaperon complex after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506885	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H187 cells assessed as subG1 accumulation at 5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506919	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-9 cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506891	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of caspase-3 cleavage at 10 uM after 72 hrs by fluorescence assay in presence of caspase-9 inhibitor Z-LEHD-FMK	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506911	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of cell growth arrest at 100 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506887	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H187 cells assessed as subG1 accumulation at 25 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506886	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H187 cells assessed as subG1 accumulation at 15 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506890	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as increase in caspase-3 activity at 10 uM after 72 hrs by fluorescence assay in presence of caspase-9 inhibitor Z-LEHD-FMK	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506875	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-N417 cells assessed as mitochondrial membrane depolarization at 5 uM after 96 hrs by JC-1 staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506872	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of PARP cleavage at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506908	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of cell growth arrest at 50 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242177	Inhibition of HSF1 in human ASB244 cells assessed as potentiation of geldanamycin-induced reduction in cell migration at 10 uM relative to geldanamycin alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506899	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as reduction in BAD phosphorylation at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506884	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H187 cells assessed as subG1 accumulation at 2.5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506912	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-3 cleavage at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506945	Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-3 cleavage after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242165	Inhibition of HSF1 in human ASB244 cells assessed as potentiation of 17-DMAG-induced reduction in cell proliferation at 20 uM relative to 17-DMAG alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506948	Inhibition of HSP70-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of caspase-3 cleavage after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506932	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of PARP cleavage at 400 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506943	Inhibition of HSP70-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of cell growth arrest after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506870	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of caspase-9 cleavage at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506871	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of caspase-2 cleavage at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506869	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as increase in caspase-3 activity at 10 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506895	Effect on HSP90-mediated survivin expression in human NCI-H526 cells at 25 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506906	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of cell growth arrest at 20 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506901	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as reduction in BAD phosphorylation at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506879	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as subG1 accumulation at 25 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242174	Inhibition of HSF1 in human HL60 cells assessed as potentiation of 17-AAG-induced increase in apoptosis at 400 uM relative to 17-AAG alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506874	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H69 cells assessed as mitochondrial membrane depolarization at 5 uM after 72 hrs by JC-1 staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506894	Effect on HSP90-mediated Bcl-XL expression in human NCI-H526 cells at 25 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506868	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H69 cells assessed as increase in apoptotic cell population at 0.2 to 1 uM after 72 hrs by FACS analysis relative to control	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506909	Inhibition of HSP90-mediated antiapoptotic activity in human MCF7 cells assessed as induction of cell growth arrest at 50 uM after 24 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506878	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as subG1 accumulation at 15 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506914	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of PARP cleavage at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506881	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-N417 cells assessed as subG1 accumulation at 5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506893	Effect on HSP90-mediated Bcl-2 expression in human NCI-H526 cells at 25 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506876	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as subG1 accumulation at 2.5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242175	Inhibition of HSF1 in human ASB145 cells assessed as potentiation of geldanamycin-induced reduction in cell proliferation at 20 uM relative to geldanamycin alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID1242176	Inhibition of HSF1 in human ASB244 cells assessed as potentiation of geldanamycin-induced reduction in cell proliferation at 20 uM relative to geldanamycin alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506896	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as release of Apaf-1 from chaperon complex at 20 uM after 1 hr by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506913	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-9 cleavage at 20 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID1242173	Inhibition of HSF1 in human HL60 cells assessed as potentiation of 17-AAG-induced reduction in cologenicity at 400 uM relative to 17-AAG alone	2015	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17	Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.
AID506915	Inhibition of HSP90-mediated antiapoptotic activity in human SKBR3 cells assessed as induction of caspase-3 cleavage at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506873	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H187 cells assessed as mitochondrial membrane depolarization at 5 uM after 72 hrs by JC-1 staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506892	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as induction of PARP cleavage at 10 uM after 72 hrs by fluorescence assay in presence of caspase-9 inhibitor Z-LEHD-FMK	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506880	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-N417 cells assessed as subG1 accumulation at 2.5 uM after 72 hrs by propidium iodide staining-based flow cytometry	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506888	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as mitochondrial membrane depolarization at 10 uM after 72 hrs by JC-1 staining-based flow cytometry in presence of broad-spectrum caspase inhibitor Boc-D-FMK	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
AID506905	Inhibition of HSP90-mediated antiapoptotic activity in human NCI-H526 cells assessed as disruption of protein-Apaf-1 complex at 50 uM after 24 hrs by Western blot analysis	2007	Nature chemical biology, Aug, Volume: 3, Issue:8	Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	19 (32.20)	29.6817
2010's	36 (61.02)	24.3611
2020's	4 (6.78)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (1.64%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	60 (98.36%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
niacinamide nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.	2.08	1	pyridine alkaloid; pyridinecarboxamide; vitamin B3	anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor
phosphorylcholine Phosphorylcholine: Calcium and magnesium salts used therapeutically in hepatobiliary dysfunction.. phosphocholine : The phosphate of choline; and the parent compound of the phosphocholine family.	2.08	1	phosphocholines	allergen; epitope; hapten; human metabolite; mouse metabolite
valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.	2.47	2	branched-chain fatty acid; branched-chain saturated fatty acid	anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent
ebselen ebselen : A benzoselenazole that is 1,2-benzoselenazol-3-one carrying an additional phenyl substituent at position 2. Acts as a mimic of glutathione peroxidase.	2.03	1	benzoselenazole	anti-inflammatory drug; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 3.5.4.1 (cytosine deaminase) inhibitor; EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor; enzyme mimic; ferroptosis inhibitor; genotoxin; hepatoprotective agent; neuroprotective agent; radical scavenger
vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).	2.17	1	dicarboxylic acid diamide; hydroxamic acid	antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor
glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.	2.13	1	amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid	EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
methylene blue Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.	2.1	1	organic chloride salt	acid-base indicator; antidepressant; antimalarial; antimicrobial agent; antioxidant; cardioprotective agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 4.6.1.2 (guanylate cyclase) inhibitor; fluorochrome; histological dye; neuroprotective agent; physical tracer
cytarabine [no description available]	2.02	1	beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside	antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent
rotenone Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.	2.02	1	organic heteropentacyclic compound; rotenones	antineoplastic agent; metabolite; mitochondrial NADH:ubiquinone reductase inhibitor; phytogenic insecticide; piscicide; toxin
4-butyrolactone 4-Butyrolactone: One of the FURANS with a carbonyl thereby forming a cyclic lactone. It is an endogenous compound made from gamma-aminobutyrate and is the precursor of gamma-hydroxybutyrate. It is also used as a pharmacological agent and solvent.. tetrahydrofuranone : Any oxolane having an oxo- substituent at any position on the tetrahydrofuran ring.. gamma-butyrolactone : A butan-4-olide that is tetrahydrofuran substituted by an oxo group at position 2.	2.11	1	butan-4-olide	metabolite; neurotoxin
thiazoles [no description available]	2.46	2	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
pyrazines Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.	2.07	1	diazine; pyrazines	Daphnia magna metabolite
deoxycytidine [no description available]	2.06	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
arsenic trioxide Arsenic Trioxide: An inorganic compound with the chemical formula As2O3 that is used for the treatment of ACUTE PROMYELOCYTIC LEUKEMIA in patients who have relapsed from, or are resistant to, conventional drug therapy.	2.46	2
cadmium chloride Cadmium Chloride: A cadmium halide in the form of colorless crystals, soluble in water, methanol, and ethanol. It is used in photography, in dyeing, and calico printing, and as a solution to precipitate sulfides. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed). cadmium dichloride : A cadmium coordination entity in which cadmium(2+) and Cl(-) ions are present in the ratio 2:1. Although considered to be ionic, it has considerable covalent character to its bonding.	2.76	3	cadmium coordination entity
etoposide [no description available]	2.02	1	beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound	antineoplastic agent; DNA synthesis inhibitor
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	2.06	1	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
thiazolyl blue thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium.	2.03	1	organic bromide salt	colorimetric reagent; dye
alkannin alkannin: a naphthazarin used to promote wound healing, from the plant Alkanna tinctoria; RN given refers to (S)-isomer; structure	2.07	1	hydroxy-1,4-naphthoquinone
triptolide [no description available]	3.21	1	diterpenoid; epoxide; gamma-lactam; organic heteroheptacyclic compound	antispermatogenic agent; plant metabolite
celastrol [no description available]	2.77	3	monocarboxylic acid; pentacyclic triterpenoid	anti-inflammatory drug; antineoplastic agent; antioxidant; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Hsp90 inhibitor; metabolite
perifosine [no description available]	2.08	1	ammonium betaine; phospholipid	EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	2.05	1	amino acid zwitterion; angiotensin II	human metabolite
sb 203580 [no description available]	2.03	1	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent
sorafenib [no description available]	2.08	1	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor
pifithrin mu 2-phenylacetylenesulfonamide: induces p53-independent apoptotic killing of B-chronic lymphocytic leukemia cells; also inhibits Hsp70 and autophagy	2.1	1	benzenes
bortezomib [no description available]	2.49	2	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor
leupeptins Leupeptins: A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.	2.77	3
lithium chloride Lithium Chloride: A salt of lithium that has been used experimentally as an immunomodulator.. lithium chloride : A metal chloride salt with a Li(+) counterion.	2.03	1	inorganic chloride; lithium salt	antimanic drug; geroprotector
sodium arsenite sodium arsenite : An inoganic sodium salt with formula with formula NaAsO2.	2.96	4	arsenic molecular entity; inorganic sodium salt	antibacterial agent; antifungal agent; antineoplastic agent; carcinogenic agent; herbicide; insecticide; rodenticide
benzyloxycarbonylleucyl-leucyl-leucine aldehyde benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.	2.77	3	amino aldehyde; carbamate ester; tripeptide	proteasome inhibitor
arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.	2.05	1	vasopressin	cardiovascular drug; hematologic agent; mitogen
curcumin Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.	2.06	1	aromatic ether; beta-diketone; diarylheptanoid; enone; polyphenol	anti-inflammatory agent; antifungal agent; antineoplastic agent; biological pigment; contraceptive drug; dye; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.1.1.25 (shikimate dehydrogenase) inhibitor; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; EC 1.8.1.9 (thioredoxin reductase) inhibitor; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; flavouring agent; food colouring; geroprotector; hepatoprotective agent; immunomodulator; iron chelator; ligand; lipoxygenase inhibitor; metabolite; neuroprotective agent; nutraceutical; radical scavenger
dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).	2.08	1	1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor
alpha-chymotrypsin Chymotrypsin: A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.	2.07	1
naphthoquinones Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.	2.07	1
d 609 [no description available]	2.07	1
quercetin [no description available]	4.24	5	7-hydroxyflavonol; pentahydroxyflavone	antibacterial agent; antineoplastic agent; antioxidant; Aurora kinase inhibitor; chelator; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; geroprotector; phytoestrogen; plant metabolite; protein kinase inhibitor; radical scavenger
geranylgeranylacetone geranylgeranylacetone: structure in first source; RN given refers to isomeric cpd without isomeric designation; mixture of (5E,9E,13E) & (5Z,9E,13E)-isomers. teprenone : A terpene ketone in which a (9E,13E)-geranylgernayl group is bonded to one of the alpha-methyls of acetone (it is a mixture of 5E- and 5Z-geoisomers in a 3:2 ratio).	2.1	1
brefeldin a [no description available]	2.08	1	macrolide antibiotic	Penicillium metabolite
17-(dimethylaminoethylamino)-17-demethoxygeldanamycin 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: structure in first source. alvespimycin : A 19-membered macrocyle that is geldanamycin in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group.	2.44	2	1,4-benzoquinones; ansamycin; carbamate ester; secondary amino compound; tertiary amino compound	Hsp90 inhibitor
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.55	2	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
herbimycin herbimycin: herbicidal antibiotic produced by Streptomyces sp.; see also herbimycin B; structure for herbimycin A in second source. herbimycin : A 19-membered macrocyle incorporating a benzoquinone ring and a lactam functionality. It is an ansamycin antibiotic that induces apoptosis and displays antitumour effects.	2.04	1	1,4-benzoquinones; lactam; macrocycle	antimicrobial agent; apoptosis inducer; herbicide; Hsp90 inhibitor; tyrosine kinase inhibitor
ligustilide ligustilide: found in Umbelliferae plants; RN given refers to cpd without isomeric designation; structure in first source	2.11	1	butenolide	metabolite
casein kinase ii Casein Kinase II: A ubiquitous casein kinase that is comprised of two distinct catalytic subunits and dimeric regulatory subunit. Casein kinase II has been shown to phosphorylate a large number of substrates, many of which are proteins involved in the regulation of gene expression.	2.07	1
arsenic Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed)	2.46	2	metalloid atom; pnictogen	micronutrient
monorden monorden: inhibits HSP90 Heat-Shock Proteins, DNA topoisomerase VI and human Topoisomerase II	2.03	1	cyclic ketone; enone; epoxide; macrolide antibiotic; monochlorobenzenes; phenols	antifungal agent; metabolite; tyrosine kinase inhibitor
tetrodotoxin Tetrodotoxin: An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.. tetrodotoxin : A quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.	2.13	1	azatetracycloalkane; oxatetracycloalkane; quinazoline alkaloid	animal metabolite; bacterial metabolite; marine metabolite; neurotoxin; voltage-gated sodium channel blocker
selenium Selenium: An element with the atomic symbol Se, atomic number 34, and atomic weight 78.97. It is an essential micronutrient for mammals and other animals but is toxic in large amounts. Selenium protects intracellular structures against oxidative damage. It is an essential component of GLUTATHIONE PEROXIDASE.	2.03	1	chalcogen; nonmetal atom	micronutrient
tanespimycin CP 127374: analog of herbimycin A	2.73	3	1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound	antineoplastic agent; apoptosis inducer; Hsp90 inhibitor
9h-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-n-(1-methylethyl)- 9H-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-N-(1-methylethyl)-: an epichaperome (purine-scaffold) inhibitor; structure in first source	2.03	1
cycloproparadicicol cycloproparadicicol: structure in first source	2.03	1
incb-018424 [no description available]	2.08	1	nitrile; pyrazoles; pyrrolopyrimidine	antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
interleukin-8 Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.	2.13	1
pf-670462 PF-670462: inhibitor of casein kinase I epsilon; structure in first source. PF-670462 : A hydrochloride salt resulting from the formal reaction of 3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine with 2 mol eq. of hydrogen chloride. It is a selective inhibitor of the delta- and epsilon-isoforms of casein kinase 1 (CK1delta and CK1epsilon).	2.13	1	hydrochloride	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
vasoactive intestinal peptide Vasoactive Intestinal Peptide: A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE).	2.05	1
n2-(1h-indazole-5-yl)-n6-methyl-3-nitropyridine-2,6-diamine N2-(1H-indazole-5-yl)-N6-methyl-3-nitropyridine-2,6-diamine: a heat shock factor 1 antagonist; structure in first source. KRIBB11 : A member of the class of indazoles that is 1H-indazole substituted by a [6-(methylamino)-3-nitropyridin-2-yl]amino group at position 5. It is an inhibitor of heat shock factor 1 (IC50 = 1.2muM) and suppresses tumour growth in mouse xenograft models.	3.21	1
akt-i-1,2 compound Akt-I-1,2 compound: an aminopeptidase P inhibitor; structure in first source	2.03	1
deoxyguanosine [no description available]	2.03	1	purine 2'-deoxyribonucleoside; purines 2'-deoxy-D-ribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
trypan blue Trypan Blue: A diazo-naphthalene sulfonate that is widely used as a stain.. trypan blue : An organosulfonate salt that is the tetrasodium salt of 3,3'-[(3,3'-dimethylbiphenyl-4,4'-diyl)didiazene-2,1-diyl]bis(5-amino-4-hydroxynaphthalene-2,7-disulfonic acid).	2.05	1
8-hydroxy-2'-deoxyguanosine 8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.	2.03	1	guanosines	biomarker

Condition	Relationship Strength	Studies
Carcinoma, Oat Cell [description not available]	2.03	1
Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.	2.03	1
Cancer of Lung [description not available]	2.74	3
Lung Neoplasms Tumors or cancer of the LUNG.	2.74	3
Carcinoma, Small Cell An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)	2.03	1
Benign Neoplasms [description not available]	3.72	3
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.72	3
Metastase [description not available]	2.25	1
Colorectal Cancer [description not available]	2.25	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.25	1
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	2.25	1
ALS - Amyotrophic Lateral Sclerosis [description not available]	2.25	1
Nerve Degeneration Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.	2.25	1
Amyotrophic Lateral Sclerosis A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94)	2.25	1
Peritoneal Carcinomatosis [description not available]	2.15	1
Cancer of Stomach [description not available]	2.15	1
Peritoneal Neoplasms Tumors or cancer of the PERITONEUM.	2.15	1
Stomach Neoplasms Tumors or cancer of the STOMACH.	2.15	1
Hepatitis B Virus Infection [description not available]	2.15	1
Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	2.15	1
Chronic Illness [description not available]	2.45	2
Erythremia [description not available]	2.08	1
Hemorrhagic Thrombocythemia [description not available]	2.08	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.45	2
Myeloproliferative Disorders Conditions which cause proliferation of hemopoietically active tissue or of tissue which has embryonic hemopoietic potential. They all involve dysregulation of multipotent MYELOID PROGENITOR CELLS, most often caused by a mutation in the JAK2 PROTEIN TYROSINE KINASE.	2.08	1
Polycythemia Vera A myeloproliferative disorder of unknown etiology, characterized by abnormal proliferation of all hematopoietic bone marrow elements and an absolute increase in red cell mass and total blood volume, associated frequently with splenomegaly, leukocytosis, and thrombocythemia. Hematopoiesis is also reactive in extramedullary sites (liver and spleen). In time myelofibrosis occurs.	2.08	1
Thrombocythemia, Essential A clinical syndrome characterized by repeated spontaneous hemorrhages and a remarkable increase in the number of circulating platelets.	2.08	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.76	3
Cardiac Diseases [description not available]	2.1	1
Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities.	2.1	1
Kahler Disease [description not available]	2.48	2
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	2.48	2
Cerebral Infarction, Middle Cerebral Artery [description not available]	2.11	1
Injury, Ischemia-Reperfusion [description not available]	2.11	1
Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.	2.11	1
Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.	2.11	1
Endotoxin Shock [description not available]	2.13	1
Shock, Septic Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.	2.13	1
Grippe [description not available]	2.13	1
Influenza, Human An acute viral infection in humans involving the respiratory tract. It is marked by inflammation of the NASAL MUCOSA; the PHARYNX; and conjunctiva, and by headache and severe, often generalized, myalgia.	2.13	1
Anoxemia [description not available]	2.13	1
Hypoxia Sub-optimal OXYGEN levels in the ambient air of living organisms.	2.13	1
Ischemia A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.	2.05	1
Cardiac Remodeling, Ventricular [description not available]	2.05	1
Cirrhosis [description not available]	2.05	1
Cardiac Hypertrophy Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.	2.05	1
Blood Pressure, High [description not available]	2.05	1
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	2.05	1
Cardiomegaly Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.	2.05	1
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	2.05	1
Glial Cell Tumors [description not available]	2.05	1
Glioma Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)	2.05	1
Cancer of Pancreas [description not available]	2.06	1
Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).	2.06	1
Cancer of Prostate [description not available]	2.06	1
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	2.06	1
Astrocytoma, Grade IV [description not available]	2.45	2
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	2.45	2
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	2.06	1
Acoustic Neurinoma, Bilateral [description not available]	2.06	1
Neurofibromatosis 2 An autosomal dominant disorder characterized by a high incidence of bilateral acoustic neuromas as well as schwannomas (NEURILEMMOMA) of other cranial and peripheral nerves, and other benign intracranial tumors including meningiomas, ependymomas, spinal neurofibromas, and gliomas. The disease has been linked to mutations of the NF2 gene (GENES, NEUROFIBROMATOSIS 2) on chromosome 22 (22q12) and usually presents clinically in the first or second decade of life.	2.06	1
Lung Adenocarcinoma [description not available]	2.07	1
Adenocarcinoma, Basal Cell [description not available]	2.45	2
Carcinoma, Non-Small Cell Lung [description not available]	2.46	2
Angiogenesis, Pathologic [description not available]	2.07	1
Adenocarcinoma of Lung A carcinoma originating in the lung and the most common lung cancer type in never-smokers. Malignant cells exhibit distinct features such as glandular epithelial, or tubular morphology. Mutations in KRAS, EGFR, BRAF, and ERBB2 genes are associated with this cancer.	2.07	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	2.45	2
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	2.46	2
Cancer of Esophagus [description not available]	2.01	1
Esophageal Neoplasms Tumors or cancer of the ESOPHAGUS.	2.01	1
Carcinoma, Epidermoid [description not available]	2.02	1
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.02	1
Acute Myelogenous Leukemia [description not available]	2.02	1
Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.	2.02	1
Hypothermia, Accidental [description not available]	2.02	1
Hypothermia Lower than normal body temperature, especially in warm-blooded animals.	2.02	1
Cardiovascular Stroke [description not available]	2.03	1
Injury, Myocardial Reperfusion [description not available]	2.03	1
Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).	2.03	1
Neoplasms, Squamous Cell Neoplasms of the SQUAMOUS EPITHELIAL CELLS. The concept does not refer to neoplasms located in tissue composed of squamous elements.	2.03	1
Cancer of Mouth [description not available]	2.03	1
Mouth Neoplasms Tumors or cancer of the MOUTH.	2.03	1
Pyrexia [description not available]	2.42	2
Fever An abnormal elevation of body temperature, usually as a result of a pathologic process.	2.42	2
Cancer of Colon [description not available]	2	1
Colonic Neoplasms Tumors or cancer of the COLON.	2	1

knk 437

Description

Cross-References

Synonyms (10)

Research Excerpts

Compound-Compound Interactions

Bioassays (71)

Research

Studies (59)

Market Indicators

Research Demand Index: 17.20

Study Types

knk 437

Description

Cross-References

Synonyms (10)

Research Excerpts

Compound-Compound Interactions

Bioassays (71)

Research

Studies (59)

Market Indicators

Research Demand Index: 17.20

Study Types

Related Drugs (61)

Related Conditions (86)