CCT018159

SKU: orb1704937

Description

CCT018159 is a 3,4-diarylpyrazole resorcinol-based, ATP-competitive HSP90 inhibitor with IC50 values of 3.2 μM (human Hsp90β) and 6.6 μM (yeast Hsp90). It suppresses tumor angiogenesis and invasion by inhibiting key endothelial and tumor cell functions, leading to G1 cell cycle arrest and apoptosis in vitro.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 171009-07-7
• MW: 352.38
• Purity: 99.79%
• Formula: C₂₀H₂₀N₂O₄
• SMILES: CC1=C(C(=NN1)C2=CC(CC)=C(O)C=C2O)C=3C=C4C(=CC3)OCCO4
• Target: HSP,Apoptosis
• Solubility: DMSO:112.5 mg/mL (319.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.35 mM)

Bioactivity

• Target IC50:
  HSP90:3.2 µM|HSP90 (yeast):6.6 μM|HSP90 β (human):3.2 μM
• In Vivo:
  CCT018159 (4 mg/mouse; s.c.; ones daily for 14 days; AtT-20-xenografted mice) reduced tumor weight compared to AtT-20-xenografted control mice. CCT018159 also decreased plasma ACTH levels, and POMC and PTTG1 mRNA levels in the tumor cells.
• In Vitro:
  CCT018159 (100 nM-10 μM) decreased POMC mRNA levels in AtT-20 cells and ACTH levels in the culture medium of these cells, suggesting that CCT018159 suppresses ACTH synthesis and secretion in corticotroph tumor cells. CCT018159 also decreased cell proliferation and induced apoptosis. FACS analyses revealed that CCT018159 agents increased the percentage of AtT-20 cells in the G2/M phase. CCT018159 decreased cell proliferation, presumably due to the induction of cell death and arrest of the cell cycle in AtT-20 cells.

Storage & Handling

• Storage: store at low temperature | 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

CCT018159, CCT-018159, CCT 018159, apoptosis, HSP90

Compound Identifiers

PubChem CID

984170