CW069

SKU: orb1222639

Description

CW069 is an allosteric inhibitor of HSET. CW069 showed marked activity against HSET in vitro. The inhibitor induced multipolar mitoses only in cells containing supernumerary centrosomes. CW069 therefore constitutes a valuable tool for probing HSET function and, by reducing the growth of cells containing supernumerary centrosomes, paves the way for new cancer therapeutics.

Key Properties

• CAS Number: 1594094-64-0
• MW: 500.33
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₁IN₂O₃
• SMILES: O=C(O)c1cc(I)ccc1NC(=O)[C@@H](NCc1ccccc1)Cc1ccccc1
• Target: HSET
• Solubility: DMSO : ≥ 52 mg/mL; 103.93 mM

Bioactivity

• In Vitro:
  CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM. CW-069 shows statistically significant selectivity over KSP. CW-069 potently suppresses N1E-115 cells, and less potently inhibits the NHDF cells, with IC50 of 86 ± 10 μM and 181 ± 7 μM, respectively. CW-069 (100 or 200 μM) causes increased multipolar spindles in N1E-115 cells with supernumerary centrosomes and shows no effect on altering bipolar spindle morphology in normal human dermal fibroblast cells. CW-069 (200 μM) cacuses multipolar anaphase and cell death induced in N1E-115 cells via transfection with HSET siRNA, and antagonizes inhibition of KSP by monastrol, but does not exert mitotic arrest in HeLa cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CW069 | CW-069 | CW 069

Quick Database Links

Gene Symbol

HSET