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ICG-001 is a small molecule inhibitor of beta-catenin/cyclic AMP responsive element binding protein (CREB) binding protein (CBP)-mediated transcription (IC50 = 3 µM). By binding CBP, thus blocking interaction with beta-catenin, it selectively induces apoptosis in transformed colon cells but not in normal cells and prevents the growth of colon carcinoma cells at 25 µM in vitro. ICG-001 has been used to specifically disrupt the beta-catenin pathway in studying epithelial-mesenchymal transition during pulmonary fibrosis. Additionally, ICG-001 disruption of Wnt/beta-catenin signaling has been studied in the context of regulating cancer stem cells.Formal Name: (6S,9aS)-hexahydro-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide. CAS Number: 780757-88-2. Molecular Formula: C33H32N4O4. Formula Weight: 548.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 224, 280 nm. SMILES: O=C([C@H](CC1=CC=C(O)C=C1)N(C(CCN2C(NCC3=CC=CC=C3)=O)=O)[C@]2([H])C4)N4CC5=CC=CC6=CC=CC=C65. InChi Code: InChI=1S/C33H32N4O4/c38-27-15-13-23(14-16-27)19-29-32(40)35(21-26-11-6-10-25-9-4-5-12-28(25)26)22-30-36(18-17-31(39)37(29)30)33(41)34-20-24-7-2-1-3-8-24/h1-16,29-30,38H,17-22H2,(H,34,41)/t29-,30+/m0/s1. InChi Key: HQWTUOLCGKIECB-XZWHSSHBSA-N.
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