THZ 531
THZ 531 (THZ531) is a first-in-class, selective CDK12 and CDK13 covalent inhibitor with IC50 of 158 nM and 69 nM, respectively; dispalys 50-fold selectivity over CDK7 and CDK9 (IC50 of 8.5 and 10.5 uM, respectively), and shows no appreciable inhibitory effect on ERK1; irreversiblely inhibits Jurkat cell proliferation with an IC50 of 50 nM, induces apoptosis in a dose- and time-dependent manner with low doses (<350 nM) ; selectively reduced Ser2 phosphorylation levels without appreciable effect on CTD pSer5/pSer7 levels, causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II, inhibits DDR and transcription factor gene expression.
Product Specifications
CAS Number
1702809-17-3
Product Name Alternative
THZ531
Purity
>98% (HPLC)
Solubility
DMSO: Soluble (< 1 mg/ml refers to the product slightly soluble or insoluble)
Smiles
O=C (NC1=CC=C (C (N2C[C@H] (NC3=NC=C (Cl) C (C4=CNC5=C4C=CC=C5) =N3) CCC2) =O) C=C1) /C=C/CN (C) C
Molecular Formula
C30H32ClN7O2
Molecular Weight
558.083
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(R, E) -N- (4- (3- ((5-chloro-4- (1H-indol-3-yl) pyrimidin-2-yl) amino) piperidine-1-carbonyl) phenyl) -4- (dimethylamino) but-2-enamide
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