CDK12-IN-2


CAS No. : 2244987-03-7

2244987-03-7
Price and Availability of CAS No. : 2244987-03-7
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5mg $280 In-stock
10mg $490 In-stock
25mg $790 In-stock
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100mg $1520 In-stock
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Cat. No. : HY-112626
M.Wt: 532.64
Formula: C32H32N6O2
Purity: >98 %
Solubility: DMSO : 50 mg/mL (ultrasonic;warming;heat to 60°C)
Introduction of 2244987-03-7 :

CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12[1]. In Vitro: CDK12-IN-2 inhibits the phosphorylation of the CTD Ser2 in SK-BR-3 cells at low submicromolar concentrations, it inhibits C-terminal domain ser2 phosphorylation with an IC50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC50 of 0.8 μM in SK-BR-3 cells[1].
CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC50 value for CDK12-IN-2 are 0.0078 μM, 0.042 μM, 0.057 μM,and 0.059 μM, for 0h, 1h, 2h and 5h respectively[1].

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