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THZ531 is a covalent CDK12 and CDK13 inhibitor with IC50 values of 158 nM and 69 nM, respectively. THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes.
*This compound is unstable in solutions, freshly prepared is recommended.
Molecular Weight | 558.07 |
Formula | C30H32ClN7O2 |
CAS Number | 1702809-17-3 |
Solubility (25°C) | DMSO ≥ 12 mg/mL |
Storage | -20°C, dry, sealed, protect from light |
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