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THZ531

Catalog No. T4293   CAS 1702809-17-3

THZ531 is a covalent inhibitor of both CDK12(IC50=158 nM) and CDK13(IC50=69 nM).

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THZ531 Chemical Structure
THZ531, CAS 1702809-17-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 57.00
2 mg In stock $ 83.00
5 mg In stock $ 113.00
10 mg In stock $ 155.00
25 mg In stock $ 347.00
50 mg In stock $ 497.00
100 mg In stock $ 723.00
500 mg In stock $ 1,490.00
1 mL * 10 mM (in DMSO) In stock $ 139.00
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Purity: 97.17%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Solubility Information

DMSO: 45 mg/mL (80.63 mM)

TargetMolReferences and Literature

1. Zhang T, et al. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016 Oct;12(10):876-84.

TargetMolCitations

1. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 2. Qiu M, Yin Z, Wang H, et al.CDK12 and Integrator-PP2A complex modulates LEO1 phosphorylation for processive transcription elongation.Science Advances.2023, 9(20): eadf8698.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Active Compound Library Inhibitor Library Bioactive Compound Library NO PAINS Compound Library Anti-Pancreatic Cancer Compound Library Covalent Inhibitor Library Anti-Alzheimer's Disease Compound Library Anti-Breast Cancer Compound Library

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Keywords

THZ531 1702809-17-3 Cell Cycle/Checkpoint CDK inhibit Cyclin dependent kinase THZ 531 THZ-531 Inhibitor inhibitor

 

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