Promotional price valid on web orders only. Your contract pricing may differ. Interested in signing up for a dedicated account number?
Learn More
Learn More
MilliporeSigma™ Calbiochem™ Cdk7 Inhibitor VIII, THZ1
A cell-permeable, non-toxic, phenylaminopyrimidinyl-acrylamide compound that acts as a highly potent, selective, ATP-site directed, and irreversible inhibitor of Cdk7 (IC50
Supplier: MilliporeSigma™ 5.32372.0001
Description
A cell-permeable, non-toxic, phenylaminopyrimidinyl-acrylamide compound that acts as a highly potent, selective, ATP-site directed, and irreversible inhibitor of Cdk7 (IC50 = 3.2nM). Acts by allosterically and covalently modifying Cys312 located outside the canonical kinase domain. Shown to block the phosphorylation of Ser5 and Ser7 in RNAPII CTD, the intracellular substrate of Cdk7 (< 250 nM, 4 h in Jurkat cells). Does not affect the activity of C312S mutated Cdk7. Exhibits comparatively week activity towards Cdk12 (IC50 = 250nM), Cdk1, and Cdk2. Suppresses the proliferation and cell viability of T-ALL and CLL cell lines and induces apoptosis with significant reduction in the levels of MCL-1 and XIAP. Also induces a significant reduction in the transcript and protein levels of RUNX1, TAL, and GATA3 (∽ 50nM). Suppresses the growth of KOPTK1 cells xenografts in murine model (10mg/kg, b.i.d).Please note that the molecular weight for this compound is batch-specific due to variable water content.
Specifications
Yellow | |
Cdk7 | |
DMSO | |
Solid |
96% by HPLC | |
C31H28ClN7O2·4HCl | |
Hygroscopic, Protect from light | |
10 mg |
Provide Content Correction
We continue to work to improve your shopping experience and your feedback regarding this content is very important to us. Please use the form below to provide feedback related to the content on this product.
Product Title
Spot an opportunity for improvement?
Provide Content Correction