1189558-88-0
Chemical Structure
CDKI-83
- CAS No.: 1189558-88-0
- Formula:C21H23N7O3S2
- Molecular Weight:485.58
IUPAC Name: 4-(4-methyl-2-(methylamino)thiazol-5-yl)-2-((4-methyl-3-(morpholinosulfonyl)phenyl)amino)pyrimidine-5-carbonitrile
InChIKey: SSEDQERECATUBR-UHFFFAOYSA-N
SMILES: N#CC1=CN=C(N=C1C2=C(N=C(S2)NC)C)NC3=CC=C(C(S(=O)(N4CCOCC4)=O)=C3)C
Biological Activity: 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].
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CDKI-83 | 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. | |||||||||||||||||||||
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Keywords
