Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | CDK7 (cell-based assay):3.2 nM |
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 [1]. |
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 [1]. |
細胞研究 | 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. |
別名 | THZ1 2HCl, THZ1 Dihydrochloride |
分子量 | 638.98 |
分子式 | C31H30Cl3N7O2 |
CAS No. | 2095433-94-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6.39 mg/mL (10 mM)
You can also refer to dose conversion for different animals. 詳細
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THZ1 2HCl 2095433-94-4 Cell Cycle/Checkpoint CDK THZ 1 Dihydrochloride THZ 1 THZ1 THZ1 Dihydrochloride THZ-1 Dihydrochloride THZ-1 Inhibitor inhibitor inhibit