Powder: -20°C for 3 years | In solvent: -80°C for 1 year
THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).
説明 | THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM). |
ターゲット&IC50 | CDK12:158 nM, CDK13:69 nM |
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). |
キナーゼ試験 | Cells are treated with THZ531 for 6 hours.After treatment cells are washed 2-fold with cold PBS and then lysed in the following lysis buffer: Hepes(50 mM, pH 7.4), NaCl(150 mM), 1% Nonidet P40 substitute, EDTA(5 mM), DTT(1 mM), and protease/phosphatase cocktails.Lysates are treated with bio-THZ1 or bio-TH531 for pulldown overnight at 4°C. |
細胞研究 | 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. |
分子量 | 558.07 |
分子式 | C30H32ClN7O2 |
CAS No. | 1702809-17-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (80.63 mM)
You can also refer to dose conversion for different animals. 詳細
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THZ531 1702809-17-3 Cell Cycle/Checkpoint CDK inhibit Cyclin dependent kinase THZ 531 THZ-531 Inhibitor inhibitor