化合物THZ531 T4293

Product Introduction
Bioactivity


英文名: THZ531

描述: THZ531 是一种选择性CDK12和CDK13共价抑制剂，IC50值分别为 158 nM 和 69 nM。

细胞实验: 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.

激酶实验: 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.

体外活性: 在Jurkat细胞中，THZ531（IC50=50 nM）的处理显著且不可逆地降低了细胞的增殖能力。THZ531强效抑制CDK12（IC50=158 nM）和CDK13（IC50=69 nM）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (80.63 mM)


关键字: inhibit | CDK | Cyclin dependent kinase | THZ 531 | THZ531 | THZ-531 | Inhibitor

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