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ICG-001

ICG-001

  • CAT Number: I005073
  • CAS Number: 847591-62-2
  • Molecular Formula: C₃₃H₃₂N₄O₄
  • Molecular Weight: 548.63
  • Purity: ≥95%
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ICG-001(CAT: I005073) is a small molecule that functions as an antagonist of the Wnt/β-catenin/TCF signaling pathway. It specifically binds to the CREB-binding protein (CBP) and inhibits its interaction with β-catenin, thereby disrupting the formation of transcriptional activation complexes. ICG-001 has an IC50 of 3 μM for CBP binding but does not affect the related transcriptional coactivator p300. By antagonizing the Wnt/β-catenin/TCF pathway, ICG-001 can modulate gene expression regulated by this pathway and has potential therapeutic implications in diseases where aberrant Wnt signaling is involved, such as cancer and other disorders.

Catalog Number I005073
CAS Number 847591-62-2
Molecular Formula

C₃₃H₃₂N₄O₄

Purity 95%
Target Wnt/β-catenin
Solubility DMSO ≥106mg/mL Water <1.2mg/mL Ethanol ≥42mg/mL
Storage Store at -20°C
IC50 3 uM
InChI 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
InChIKey HQWTUOLCGKIECB-XZWHSSHBSA-N
SMILES C1CN(C2CN(C(=O)C(N2C1=O)CC3=CC=C(C=C3)O)CC4=CC=CC5=CC=CC=C54)C(=O)NCC6=CC=CC=C6
Reference

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1:The β-catenin/CBP-antagonist ICG-001 inhibits pediatric glioma tumorigenicity in a Wnt-independent manner. Wiese M, Walther N, Diederichs C, Schill F, Monecke S, Salinas G, Sturm D, Pfister SM, Dressel R, Johnsen SA, Kramm CM.Oncotarget. 2017 Apr 18;8(16):27300-27313. doi: 10.18632/oncotarget.15934. PMID: 28460484 Free PMC Article<br />
2:Indocyanine Green-001 (ICG-001) Attenuates Wnt/β-catenin-induces Myocardial Injury Following Sepsis. Yousif NG, Hadi NR, Hassan AM.J Pharmacol Pharmacother. 2017 Jan-Mar;8(1):14-20. doi: 10.4103/jpp.JPP_153_16. PMID: 28405131 Free PMC Article<br />
3:Inhibition of collagen production by ICG-001, a small molecule inhibitor for Wnt/β-catenin signaling, in skin fibroblasts. Kim KI, Jeong DS, Yoon TJ, Jung EC, Lee JH, Kim CD.J Dermatol Sci. 2017 Apr;86(1):76-78. doi: 10.1016/j.jdermsci.2017.01.005. Epub 2017 Jan 6. No abstract available. PMID: 28094100 <br />
4:Wnt/β-catenin signaling inhibitor ICG-001 enhances pigmentation of cultured melanoma cells. Kim KI, Jeong DS, Jung EC, Lee JH, Kim CD, Yoon TJ.J Dermatol Sci. 2016 Nov;84(2):160-168. doi: 10.1016/j.jdermsci.2016.08.013. Epub 2016 Aug 20. PMID: 27567978 <br />
5:Canonical Wnt pathway inhibitor ICG-001 induces cytotoxicity of multiple myeloma cells in Wnt-independent manner. Grigson ER, Ozerova M, Pisklakova A, Liu H, Sullivan DM, Nefedova Y.PLoS One. 2015 Jan 30;10(1):e0117693. doi: 10.1371/journal.pone.0117693. eCollection 2015. PMID: 25635944 Free PMC Article<br />
6:The CREB-binding protein inhibitor ICG-001 suppresses pancreatic cancer growth. Arensman MD, Telesca D, Lay AR, Kershaw KM, Wu N, Donahue TR, Dawson DW.Mol Cancer Ther. 2014 Oct;13(10):2303-14. doi: 10.1158/1535-7163.MCT-13-1005. Epub 2014 Jul 31. PMID: 25082960 Free PMC Article<br />
7:The small molecule Wnt signaling modulator ICG-001 improves contractile function in chronically infarcted rat myocardium. Sasaki T, Hwang H, Nguyen C, Kloner RA, Kahn M.PLoS One. 2013 Sep 12;8(9):e75010. doi: 10.1371/journal.pone.0075010. eCollection 2013. PMID: 24069374 Free PMC Article<br />
8:ICG-001, a novel small molecule regulator of TCF/beta-catenin transcription. Eguchi M, Nguyen C, Lee SC, Kahn M.Med Chem. 2005 Sep;1(5):467-72. PMID: 16787331

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