CDK12-IN-E9 是一种有效的选择性共价 CDK12 抑制剂和非共价 CDK9 抑制剂，同时避免了 ABC 转运蛋白介导的外排。CDK12-IN-E9 对 CDK7/CyclinH 复合物的结合能力较弱，IC₅₀ > 1 μM。

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.

Solid

CDK12 CDK9/cyclinT1 23.9 nM (IC50)

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 NB and lung cancer cells, with IC50 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 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 lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Gao Y, et al. Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.

In Vitro: DMSO : 125 mg/mL (287.67 mM; Need ultrasonic)配制储备液