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.

CDK7 (cell-based assay):3.2 nM

THZ1 2HCl 不可逆地抑制RNA聚合酶II CTD的磷酸化。THZ1 2HCl(250 nM) 完全抑制CDK7底物RNAPII CTD在Ser 5和Ser 7的磷酸化，而在Jurkat细胞中Ser 2的磷酸化消失。低浓度的THZ1 2HCl对一小部分基因产生重大影响，包括RUNX1，从而导致更大基因表达程序的随后丧失，结果是细胞死亡[1]。

THZ1 2HCl在小鼠异种移植模型中抑制KOPTK1 T-ALL细胞的增殖。THZ1 2HCl(10 mg/kg)具有良好的耐受性，且其体重和行为未发生显著变化。THZ1 2HCl在动物模型中无明显毒性效应[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.