| Name | (E/Z)-THZ1 2HCl |
| Description | 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. |
| Cell Research | 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. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 6.39 mg/mL (10 mM), Sonication is recommended.
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| Keywords | THZ-1 Dihydrochloride | THZ1 Dihydrochloride | THZ1 2HCl | THZ-1 | THZ1 | THZ 1 Dihydrochloride | THZ 1 | CDK7 |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | High-Efficiency Gene Editing Small Molecule Library |
United States
