Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $57 | In Stock | |
2 mg | $83 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $347 | In Stock | |
50 mg | $497 | In Stock | |
100 mg | $723 | In Stock | |
500 mg | $1,490 | In Stock | |
1 mL x 10 mM (in DMSO) | $139 | In Stock |
Description | THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM). |
Targets&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). |
Kinase Assay | 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. |
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. |
Molecular Weight | 558.07 |
Formula | C30H32ClN7O2 |
Cas No. | 1702809-17-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (80.63 mM) ![]() | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.