Shelf life (days): 730.0
Formulation: A crystalline solid
Formal Name: (2E)-N-[4-[[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-piperidinyl]carbonyl]phenyl]-4-(dimethylamino)-2-butenamide
Purity: ≥95%
Formula Markup: C30H32ClN7O2
Formula Weight: 558.07376
CAS Number: 1702809-17-3
Notes: THZ531 is an inhibitor of cyclin-dependent kinase 12 (Cdk12) and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K, respectively).{48369} It is selective for Cdk12/cyclin K and Cdk13/cyclin K over Cdk9/cyclin T1 and Cdk7/cyclin H/MAT1 (IC50s = 10.5 and 8.5 μM, respectively). THZ531 inhibits proliferation of Jurkat cells with an IC50 value of 50 nM and induces apoptosis in a concentration-dependent manner. It also reduces expression of genes associated with the DNA damage response, including BRCA1, FANCF, and ERCC4, in Jurkat cells when used at a concentration of 50 nM.
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