THZ1 2HCl

Research use only, not for human use.

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 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.(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 .(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 .

THZ1 Dihydrochloride

Angiogenesis

CDK

CCR4

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2095433-94-4

639.0

C31H30Cl3N7O2

>98% (HPLC)

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O=C(NC1=CC=C(C(NC2=CC(NC3=NC(C4=CNC5=C4C=CC=C5)=C(Cl)C=N3)=CC=C2)=O)C=C1)C=CCN(C)C.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years