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504712 β-Catenin/Tcf Inhibitor VI, ICG-001 - CAS 847591-62-2 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (6S,9aS)-Hexahydro-6-((4-hydroxyphenyl)methyl)-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide, (6S)-N-Benzyl-6-(p-hydroxyphenylmethyl)-8-(1-naphthylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide, ICG001, Wnt Pathway Inhibitor XX

Primary Target: CREB-binding protein
504712
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
847591-62-2C₃₃H₃₂N₄O₄

Products

Catalogue NumberPackaging Qty/Pack
5.04712.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number504712
Brand Family Calbiochem®
Synonyms(6S,9aS)-Hexahydro-6-((4-hydroxyphenyl)methyl)-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide, (6S)-N-Benzyl-6-(p-hydroxyphenylmethyl)-8-(1-naphthylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide, ICG001, Wnt Pathway Inhibitor XX
References
ReferencesYan, 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.
Product Information
CAS number847591-62-2
FormOff-white powder
Hill FormulaC₃₃H₃₂N₄O₄
Chemical formulaC₃₃H₃₂N₄O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetCREB-binding protein
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.04712.0001 04055977244052

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision26-July-2013 JSW
Synonyms(6S,9aS)-Hexahydro-6-((4-hydroxyphenyl)methyl)-8-(1-naphthalenylmethyl)-4,7-dioxo-N-(phenylmethyl)-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide, (6S)-N-Benzyl-6-(p-hydroxyphenylmethyl)-8-(1-naphthylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide, ICG001, Wnt Pathway Inhibitor XX
DescriptionA cell-permeable pyrazinopyrimidinecarboxamide that competes against β-catenin for CBP (CREB-binding protein) binding (5 to 10 µM for 24 h in SW480 and C2C12 cultures) and selectively prevents CBP- but not p300-, dependent TCF/β-catenin transcriptional regulations both in cultures in vitro (5 to 25 µM in SW480, HCT116, rat RLT-6TN, and primary human IPF lung fibroblasts; 4 to 24 h) 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. 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 µM ICG-001) and be efficacious in alleviating bleomycin- (0,08 units/50 µL/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).
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number847591-62-2
Chemical formulaC₃₃H₃₂N₄O₄
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesYan, 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.