An inhibitor of Cdk12 and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K

THZ531 – 10 mg

Brand:
Cayman
CAS:
1702809-17-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 26386 - 10 mg Category:

Description

An inhibitor of Cdk12 and Cdk13 (IC50s = 158 and 69 nM for Cdk12/cyclin K and Cdk13/cyclin K, respectively); 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); inhibits proliferation of Jurkat cells (IC50 = 50 nM); induces apoptosis in Jurkat cells in a concentration-dependent manner; reduces expression of genes associated with the DNA damage response, including BRCA1, FANCF, and ERCC4, in Jurkat cells at 50 nM

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

Synonyms: 

Molecular weight: 558.1

CAS: 1702809-17-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|CDKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling||Research Area|Cancer|DNA Damage and Repair||Research Area|Immunology & Inflammation|Adaptive Immunity

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