ICG-001 Struktur

ICG-001

Bezeichnung:ICG-001

CAS-Nr847591-62-2

Englisch Name:ICG-001

CBNumberCB62520386

SummenformelC33H32N4O4

Molgewicht548.63158

MOL-Datei847591-62-2.mol

ICG-001 physikalisch-chemischer Eigenschaften

Dichte	1.37
storage temp.	+2C to +8C
Löslichkeit	Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml).
Aggregatzustand	Off-white powder
Farbe	Off-white
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

ICG-001 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
ICG-001 (847591-62-2) inhibits TCF/β-catenin mediated transcription by specifically blocking β-catenin/CBP interaction
Verwenden
(S,S)-ICG 001 is a β-turn peptidomimetic molecule inhibitor of β-catenin-Tcf-mediated transcription.
Definition
ChEBI: (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.
Allgemeine Beschreibung
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 cultures in vitro (5 to 25 μM) and in mice in 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.
Biochem/physiol Actions
Cell permeable: yes
Einzelnachweise
1) Emami?et al.?(2004),?A small molecule inhibitor of β-catenin/CREB-binding protein transcription;? Proc. Natl. Acad. Sci. USA,?101?12682 2) Zhou?et al.?(2012), Interactions?between β-catenin and transforming growth factor-β signaling pathways mediate epithelial-mesenchymal transition and are dependent on the transcription co-activator cAMP-response element-binding protein (CERB)-binding protein (CBP);??J. Biol. Chem.,?287?7026

ICG-001 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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