ICG001

SKU: orb1305968

Description

ICG001 is a selective CBP/β-catenin antagonist that inhibits Wnt-responsive transcription with an IC50 of 3 μM. It is a valuable chemical probe for studying Wnt/β-catenin signaling in cancer research and has been utilized in both cellular and animal models of tumorigenesis.

Research Area

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

Key Properties

• CAS Number: 847591-62-2
• MW: 548.63
• Purity: 99.90%
• Formula: C₃₃H₃₂N₄O₄
• SMILES: Oc1ccc(C[C@@H]2N3[C@H](CN(Cc4cccc5ccccc45)C2=O)N(CCC3=O)C(=O)NCc2ccccc2)cc1
• Target: Epigenetic Reader Domain,Wnt/beta-catenin
• Solubility: DMSO:135 mg/mL (246.07 mM);Ethanol:27.4 mg/mL (49.94 mM)

Bioactivity

• Target IC50:
  CBP:3 μM
• In Vivo:
  ICG001 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of ICG001 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of ICG001 for patients with advanced myeloid malignancies is still ongoing.
• In Vitro:
  ICG001 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with ICG001 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells.
• Cell Research:
  ICG-001 is dissolved in DMSO. To evaluate effects of ICG-001 on α-SMA and collagen type 1 expression, RLE-6TN cells are treated with TGF-β1 (0.25 ng/mL) in the presence or absence of ICG-001 (5.0 μM). After 24 h, cells are harvested and mRNA isolated for analysis by qPCR. RNA is reverse-transcribed using SuperScript reverse transcriptase. Quantitative PCR is performed with SYBR-Green PCR using Real-Time PCR System HT7900. The amplification protocol is set as follows: 95°C denaturation for 10 min followed by 40 cycles of 15-s denaturation at 95°C, 1 min of annealing/extension, and data collection at 60°C.

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

Epigenetic Reader Domain, EpigeneticReaderDomain, ICG001, ICG-001, ICG 001, CBP, beta-catenin, betacatenin, 780757-88-2, 847591-62-2, bcatenin, PRI 724, PRI724, PRI-724, PRI-724 isomer, Wnt/β-catenin, Wnt/b-catenin, Wnt/betacatenin, Wnt, βcatenin

Compound Identifiers

PubChem CID

11238147