| Identification | Back Directory | [Name]
CDK12 inhibitor E9 S-isomer | [CAS]
2020052-55-3 | [Synonyms]
CDK12-IN-E9
CDK inhibitor E9
CDK12 inhibitor E9 S-isomer | [Molecular Formula]
C24H30N6O2 | [MDL Number]
MFCD32708509 | [MOL File]
2020052-55-3.mol | [Molecular Weight]
434.53 |
| Hazard Information | Back Directory | [Description]
CDK12-IN-E9 is a covalent inhibitor of CDK12. It has been shown to overcome resistance to the THZ series of covalent transcriptional CDK Inhibitors. | [Uses]
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 IC50> 1 μM[1]. | [IC 50]
CDK12; CDK9/cyclinT1: 23.9 nM (IC50); cdk2/cyclin A: 932 nM (IC50); CDK7/Cyclin H/MNAT1: 1210 nM (IC50) | [References]
[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. DOI:10.1016/j.chembiol.2017.11.007 |
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cjbscvictory
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13348960310 13348960310 |
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www.weikeqi-biotech.com/ |
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