THZ531

SKU: orb1302979

Description

THZ531 is a potent, covalent inhibitor of CDK12 and CDK13, with IC50 values of 158 nM and 69 nM, respectively. It is a valuable chemical probe for studying transcription regulation in cancer research and has been utilized in both in vitro and in vivo experimental models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1702809-17-3
• MW: 558.07
• Purity: 99.86%
• Formula: C₃₀H₃₂ClN₇O₂
• SMILES: CN(C)C\C=C\C(=O)Nc1ccc(cc1)C(=O)N1CCC[C@H](C1)Nc1ncc(Cl)c(n1)-c1c[nH]c2ccccc12
• Target: CDK
• Solubility: DMSO:8.17 mg/mL (14.64 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.79 mM)

Bioactivity

• Target IC50:
  CDK13:69 nM|CDK9:10.5 μM|CDK12:158 nM|CDK7:8.5 μM
• In Vitro:
  In Jurkat cell, THZ531(IC50=50 nM) treatment leads to a dramatic and irreversible decrease proliferation.THZ531 potently inhibits CDK12(IC50=158 nM) and CDK13 (IC50=69 nM).
• Cell Research:
  Jurkat cells are plated in 96-well plates at 20,000 cells/well in fresh media and treated with THZ531 or DMSO at the indicated concentrations for 72 hours. HAP1 cells are seeded in 96-well plates at 12,000 cells/well in fresh media and 24 hours later are treated with THZ531 at the indicated concentrations for 72 hours. Anti-proliferative effect of THZ531 is assessed. To assess the effect of inhibitor washout on anti-proliferation of Jurkat cells, cells are treated with THZ531 or DMSO for 6 hrs. Inhibitor-containing medium is then removed and incubated with or without THZ531 for 66 hrs. Anti-proliferative effect of THZ531 is assessed. All proliferation assays are performed in biological triplicate. IC50s are determined using non-linear regression curve fit.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK, CDK13, CDK12, Cyclin dependent kinase, inhibit, Inhibitor, THZ531, THZ-531, THZ 531

Compound Identifiers

PubChem CID

118025540