(E/Z)-THZ1 2HCl

SKU: orb1304110

Description

THZ1 2HCl

Research Area

Cell Biology

Key Properties

• CAS Number: 2095433-94-4
• MW: 638.98
• Purity: 99.51%
• Formula: C₃₁H₃₀Cl₃N₇O₂
• SMILES: Cl.Cl.CN(C)C\C=C\C(=O)Nc1ccc(cc1)C(=O)Nc1cccc(Nc2ncc(Cl)c(n2)-c2c[nH]c3ccccc23)c1
• Target: CDK
• Solubility: DMSO:6.39 mg/mL (10 mM)

Bioactivity

• Target IC50:
  CDK7 (cell-based assay):3.2 nM
• 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 .
• 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 .
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK7, (E/Z)-THZ1 2HCl, (E/Z)-THZ1 Dihydrochloride, THZ 1, THZ 1 Dihydrochloride, THZ1, THZ-1, THZ1 2HCl, THZ1 Dihydrochloride, THZ-1 Dihydrochloride

Compound Identifiers

PubChem CID

129896819