| Identification | Back Directory | [Name]
CDKI-83 | [CAS]
1189558-88-0 | [Synonyms]
CDKI-83
5-Pyrimidinecarbonitrile, 4-[4-methyl-2-(methylamino)-5-thiazolyl]-2-[[4-methyl-3-(4-morpholinylsulfonyl)phenyl]amino]- | [Molecular Formula]
C21H23N7O3S2 | [MOL File]
1189558-88-0.mol | [Molecular Weight]
485.58 |
| Hazard Information | Back Directory | [Uses]
CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research[1]. | [IC 50]
CDK9/T1: 21 nM (Ki); CDK1/B: 72 nM (Ki); CDK2/E: 232 nM (Ki); CDK4/D: 290 nM (Ki); CDK7/H: 405 nM (Ki) | [References]
[1] Xiangrui Liu, et al. In vitro antitumor mechanism of a novel cyclin-dependent kinase inhibitor CDKI-83. Invest New Drugs. 2012 Jun;30(3):889-97. DOI:10.1007/s10637-011-9641-5 |
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| Company Name: |
BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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