MilliporeSigma™ Calbiochem™ Cdk7 Inhibitor VIII, THZ1

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

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

• Color: Yellow
• Description: 96% by HPLC
• Target Proteins: Cdk7
• Molecular Formula: C₃₁H₂₈ClN₇O₂·4HCl
• Solubility: DMSO
• Content And Storage: Hygroscopic, Protect from light
• Form: Solid
• Quantity: 10 mg