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Purity: ≥98%
ICG-001 (ICG001; ICG 001) is a novel and potent inhibitor of β-catenin/TCF mediated transcription. It potently and selectively antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 modulates Wnt signaling and increased the expression of genes beneficial for cardiac regeneration in epicardial cells. ICG-001 binds cAMP-responsive element binding (CREB)-binding protein (CBP) to disrupt its interaction with β-catenin and inhibit CBP function as a coactivator of Wnt/β-catenin-mediated transcription.
| ln Vitro |
In MCF7 cells, leptin-induced EMT, invasion, and tumor sphere formation are inhibited by ICG-001 (5 μM) [1]. In presenilin-1 mutant cells, ICG-001 can phenotypically rescue normal nerve growth factor (NGF)-induced neuronal differentiation and neuronal outgrowth, highlighting the significance of neuronal differentiation and the function of the TCF/β-catenin signaling pathway in neurite outgrowth [2]. In SW480 cells, the steady-state levels of survivin and cyclin D1 RNA and protein were decreased by ICG-001 (25 μM) treatment; these two proteins are increased by β-catenin. ICG-001 inhibits the development of colon cancer cells in vitro and specifically triggers apoptosis in transformed cells but not in normal colon cells [3].
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| ln Vivo |
In mice, ICG-001 (5 mg/kg daily) strongly suppresses β-catenin signaling while preserving epithelial cells [2]. The development of polyps in the colon and small intestine was reduced by 42% after 9 weeks of administration of a water-soluble version of ICG-001. This impact was comparable to that of the nonsteroidal anti-inflammatory medication MK-231, which has repeatedly demonstrated efficacy in this model. In the SW620 nude mouse tumor regression xenograft model, ICG-001 (150 mg/kg, i.v.) caused a notable reduction in tumor volume over the course of 19 days of therapy without causing death or weight loss [3].
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| References |
[1]. Yan D, et al, Leptin-induced epithelial-mesenchymal transition in breast cancer cells requires β-catenin activation via Akt/GSK3- and MTA1/Wnt1 protein-dependent pathways. J Biol Chem, 2012, 287(11), 8598-8612.
[2]. Henderson WR Jr, et al, Inhibition of Wnt/beta-catenin/CREB binding protein (CBP) signaling reverses pulmonary fibrosis. Proc Natl Acad Sci USA, 2010, 107(32), 14309-14314. [3]. Emami KH, et al. A small molecule inhibitor of beta-catenin/CREB-binding protein transcription [corrected]. Proc Natl Acad Sci USA, 2004, 101(34), 12682-12687. [4]. Liu Y, et al. ICG-001 suppresses growth of gastric cancer cells and reduces chemoresistance of cancer stem cell-like population. J Exp Clin Cancer Res. 2017 Sep 11;36(1):125 |
| Molecular Formula |
C33H32N4O4
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|---|---|
| Molecular Weight |
548.63
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| CAS # |
780757-88-2
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| Related CAS # |
1422253-38-0 (PRI-724);847591-62-2 (deleted);780757-88-2 (ICG001);
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| SMILES |
O=C1[C@]([H])(C([H])([H])C2C([H])=C([H])C(=C([H])C=2[H])O[H])N2C(C([H])([H])C([H])([H])N(C(N([H])C([H])([H])C3C([H])=C([H])C([H])=C([H])C=3[H])=O)[C@@]2([H])C([H])([H])N1C([H])([H])C1=C([H])C([H])=C([H])C2=C([H])C([H])=C([H])C([H])=C12)=O
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| InChi Key |
HQWTUOLCGKIECB-IHLOFXLRSA-N
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| 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+/m1/s1
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| Chemical Name |
rel-(6R,9aR)-Hexahydro-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
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| Synonyms |
ICG-001; ICG 001; ICG001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8227 mL | 9.1136 mL | 18.2272 mL | |
| 5 mM | 0.3645 mL | 1.8227 mL | 3.6454 mL | |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8227 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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