CDK12-IN-E9

CDK12-IN-E9

C655988-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC 50 > 1 μM In Vitro CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1 R NB and lung cancer cells, with IC 50 values ranging from 8 to 40 nM. CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression. CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1 r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells Concentration: 10 nM-10 μM Incubation Time: 72 hours Result: Showed potent antiproliferative activity in THZ1 R NB and lung cancer cells, with IC 50 values ranging from 8 to 40 nM. Western Blot AnalysisCell Line: Kelly, PC-9, and NCI-H82 cells Concentration: 0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM Incubation Time: 6 hours Result: Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1 r NB and lung cancer models. IC50& Target:CDK12 CDK9/cyclinT1 23.9 nM (IC 50 ) cdk2/cyclin A 932 nM (IC 50 ) CDK7/Cyclin H/MNAT1 1210 nM (IC 50 )

CDK12-IN-E9 是一种强效的选择性共价 CDK12 抑制剂和非共价 CDK9 抑制剂，同时可避免 ABC 转运体介导的外流。CDK12-IN-E9 与 CDK7/CyclinH 复合物的结合能力较弱，IC 50 > 1 μM。

2020052-55-3(DMSO)

C24H30N6O2

434.53 g/mol

CCC1=C2N=C(C=C(N2N=C1)NC3=CC(=CC=C3)NC(=O)C=C)N4CCCCC4CCO

包含CDK，MAPK，GSK3，CLK家族