ICG-001

SKU: orb1710780

Description

ICG001 is a selective small molecule inhibitor that disrupts the β-catenin/CBP interaction to block Wnt/β-catenin signaling, with an IC50 of 3 μM for CREB binding. It is a valuable research tool for studying oncogenic signaling in cancers, including colorectal carcinoma, in both cellular and animal models.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 780757-88-2
• MW: 548.63
• Purity: 99.59%
• Formula: C₃₃H₃₂N₄O₄
• SMILES: Oc1ccc(C[C@@H]2N3[C@H](CN(Cc4cccc5ccccc45)C2=O)N(CCC3=O)C(=O)NCc2ccccc2)cc1
• Target: Wnt/beta-catenin,Epigenetic Reader Domain,Apoptosis
• Solubility: 2% DMSO+40% PEG300+5% Tween 80+53% Saline:10 mg/mL (18.23 mM);DMSO:242 mg/mL (441.1 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:9 mg/mL (16.4 mM)

Bioactivity

• Target IC50:
  CBP:3 μM
• In Vivo:
  METHODS: In a tumor regression SW620 nude mouse xenograft model, ICG-001 (150 mg/kg, intravenous injection) was administered to observe the effect of the drug on tumor remission in nude mice. RESULTS Tumor volume was significantly reduced during the 19-day treatment, with no mortality or weight loss.
• In Vitro:
  METHODS: SW480 cells were treated with ICG-001 (25 μM, 24 h) and the inhibition of survivin gene transcription was measured by semiquantitative RT-PCR; SW480 and HCT116 cells were treated with ICG-001 (10 and 25 μM, 24 h) and analyzed by immunoblotting for survivin; SW480 cells were treated with ICG-001 (25 μM) and the chromatin immunoprecipitation assay of the cyclin D1 promoter was used; promoter occupancy was assessed with CBP- (AC-22) or p300- (C-20) specific antibodies in the presence of ICG-001 (25 μM, 8 h). RESULTS After 8 h of treatment of SW480 cells with 25 μM ICG-001, approximately 2% of the genes analyzed were upregulated by a factor greater than 2, while only approximately 0.3% of the genes were downregulated by more than 50%. The two genes downregulated were S100A4 and survivin, which are the first and fourth mRNAs upregulated in cancer cells, respectively. ICG-001 effectively reduced the steady-state levels of survivin mRNA and protein in treated colorectal cancer cells. SW480 cells treated with ICG-001 (25 μM) showed a significant decrease in cyclin D1 as early as 4 h after treatment. Using chromatin immunoprecipitation, ICG-001 was shown to selectively inhibit the endogenous cyclin D1 promoter β.

Storage & Handling

• Storage: keep away from moisture | 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

inhibit, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, ICG 001, ICG001, ICG-001, betacatenin, beta-catenin, Beta catenin, CBP, 847591-62-2, bcatenin, Apoptosis, β-catenin, βcatenin, Wnt/β-catenin, Wnt/betacatenin, Wnt/b-catenin, Wnt

Compound Identifiers

PubChem CID

11238147