β-Catenin/Tcf Inhibitor VI, ICG-001-CAS 847591-62-2-Calbiochem

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一般描述

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 ?M) 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 ?L/mouse; administered intranasally; Cat. No. 203401) induced pulmonary fibrosis in mice.
A cell-permeable pyrazinopyrimidinecarboxamide that competes against β-catenin for CBP (CREB-binding protein) binding (5 to 10 ?M for 24 h in SW480 and C2C12 cultures) and selectively prevents CBP- but not p300-, dependent TCF/β-catenin transcriptional regulations both in culturesin vitro(5 to 25 ?M in SW480, HCT116, rat RLT-6TN, and primary human IPF lung fibroblasts; 4 to 24 h) 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. Selective blockage of CBP/TCF/β-catenin complex formation by ICG-001 is shown to reactivate p300//TCF/β-catenin-mediated neuronal differentiation upon NGF stimulation in PS-1 L286V mutant-expressing PC-12 cultures (cell population with neurite outgrowth = 90% and 17% of wt PS-1 control level, respectively, with or without 10 ?M ICG-001) and be efficacious in alleviating bleomycin- (0,08 units/50 ?L/mouse; administered intranasally; Cat. No. 203401) induced pulmonary fibrosis in mice (5 mg/kg/day via osmotic pump infusion; 10 d treatment starting 1 d before bleomycin induction or 21 d treatment starting d 21 post bleomycin induction).

生化/生理作用

Cell permeable: yes
Primary Target
CREB-binding protein
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Use only fresh DMSO for reconstitution.

其他说明

Yan, D., et al. 2012.J. Biol. Chem.287,8598.
Henderson, W.R. Jr, et al. 2010.Proc. Natl. Acad. Sci. USA.107,14309.
Eguchi, M., et al. 2005.Med Chem.1,467.
Ma, H., et al. 2005.Oncogene.24,3619.
Teo, J.L., et al. 2005.Proc. Natl. Acad. Sci. USA.102,12171.
Emami, K.H., et al. 2004.Proc. Natl. Acad. Sci. USA.101,12682.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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