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THZ1 2HCl

Catalog No. T35332   CAS 2095433-94-4
Synonyms: THZ1 2HCl, THZ1 Dihydrochloride

THZ1 2HCl (THZ1 Dihydrochloride) is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.

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THZ1 2HCl Chemical Structure
THZ1 2HCl, CAS 2095433-94-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
5 mg In stock $ 92.00
10 mg In stock $ 159.00
25 mg In stock $ 362.00
50 mg In stock $ 497.00
100 mg In stock $ 672.00
200 mg In stock $ 997.00
1 mL * 10 mM (in DMSO) In stock $ 171.00
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Purity: 98.33%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description THZ1 2HCl (THZ1 Dihydrochloride) is a selective, covalent, and allosteric inhibitor of CDK7 with an IC50 of 3.2 nM. THZ1 2HCl has antiproliferative effects on a variety of cancer cell lines.
Targets&IC50 CDK7 (Cell-based assay):3.2 nM
In vitro THZ1 2HCl irreversibly inhibits the phosphorylation of RNA polymerase II CTD. THZ1 2HCl(250 nM) completely inhibits the phosphorylation of CDK7 substrate RNAPII CTD at Ser 5 and Ser 7, and the phosphorylation of Ser 2 is lost in Jurkat cells. Low concentrations of THZ1 2HCl have major effects on a small subset of genes, including RUNX1, thus leading to the subsequent loss of a larger gene expression program, resulting in cell death [1].
In vivo THZ1 2HCl inhibits the proliferation of KOPTK1 T-ALL cells in a mouse xenograft model. THZ1 2HCl(10 mg/kg) is well tolerated, and its body weight and behavior did not change significantly. THZ1 2HCl has no obvious toxic effects in animal models [1].
Cell Research Treat cells with THZ1, THZ1-R or DMSO From 0 to 6 hours, the effect of treatment time on THZ1-mediated inhibition of RNA polymerase II CTD phosphorylation was detected. In subsequent experiments, cells were treated with compounds for 4 hours, then the compound-containing medium was removed, cells were washed, and cells were grown in inhibitor-free medium.
Synonyms THZ1 2HCl, THZ1 Dihydrochloride
Molecular Weight 638.98
Formula C31H30Cl3N7O2
CAS No. 2095433-94-4

Storage

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

Solubility Information

DMSO: 6.39 mg/mL (10 mM)

TargetMolReferences and Literature

1. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20. 2. Nilson KA, et al. THZ1 Reveals Roles for Cdk7 in Co-transcriptional Capping and Pausing. Mol Cell. 2015 Aug 20;59(4):576-87.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Compound Library Bioactive Compound Library

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Rafoxanide CLK-IN-T3 AG-024322 CLK1-IN-3 THZ1-R A-674563 2HCl(552325-73-2(fb-2hcl)) (R)​-​CR8 HS-243

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Keywords

THZ1 2HCl 2095433-94-4 Cell Cycle/Checkpoint CDK THZ 1 Dihydrochloride THZ 1 THZ1 THZ1 Dihydrochloride THZ-1 Dihydrochloride THZ-1 inhibitor inhibit

 

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