THZ1 2HCl 是一种选择性、共价和变构的 CDK7 抑制剂，IC50 为 3.2 nM。 THZ1 2HCl 对多种癌细胞系具有抗增殖作用。

THZ1 2HCl 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.

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].

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].

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.

2095433-94-4

C31H30Cl3N7O2

638.97

THZ1 Dihydrochloride;THZ1二盐酸盐;THZ1 2HCl

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years