ICG 001
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ICG 001
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CAS No:
847591-62-2
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Formula:
C33H32N4O4
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Chemical Name:
ICG 001
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Synonyms:
2H-Pyrazino[1,2-a]pyriMidine-1(6H)-carboxaMide, hexahydro-6-[(4-hydroxyphenyl)Methyl]-8-(1-naphthalenylMethyl)-4,7-dioxo-N-(phenylMethyl)-, (6S,9aS)-;ICG-1;(6S,9aS)-Hexahydro-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide;ICG-001/ICG001;(6S,9aS)-Hexahydro-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide ICG001;ICG 001, >=98%;ICG-001;ICG 001;ICG001;(6S,9AS)-6-(4-hydroxybenzyl)-N-benzyl-8-(naphthalen-1-ylmethyl)-4,7-dioxo-hexahydro-2H-pyrazin
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CAS No:
Description
(6S,9aS)-6-[(4-hydroxyphenyl)methyl]-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-3,6,9,9a-tetrahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide is a peptide.
ICG-001 (847591-62-2) inhibits TCF/β-catenin mediated transcription by specifically blocking β-catenin/CBP interaction
A cell-permeable pyrazinopyrimidinecarboxamide that competes against β-catenin for CBP (CREB-binding protein) binding and selectively prevents CBP- but not p300-, dependent TCF/β-catenin transcriptional regulations both in culturesin vitro(5 to 25 μM) and in micein vivo(5 mg/kg/day via osmotic pump infusion), while not affecting CBP-dependent transcriptional activities mediated by the AP-1 or CRE complex. Shown to reactivate p300//TCF/β-catenin-mediated neuronal differentiation upon NGF stimulation in PS-1 L286V mutant-expressing PC-12 cultures and be efficacious in alleviating bleomycin- (0,08 units/50 μL/mouse; administered intranasally; Cat. No.203401) induced pulmonary fibrosis in mice.
ICG 001 Use and Manufacturing
(S,S)-ICG 001 is a β-turn peptidomimetic molecule inhibitor of β-catenin-Tcf-mediated transcription.
