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商品描述
MW:548.6Da
CASRegistry#:847591-62-2
Formula:C33H32N4O4
Background:
ICG001selectivelyinhibitscoloncarcinomacelllines(SW480andHCT-116cells)butnotnormalcolonicepithelialcells(CCD-841Co).ItisalsoefficaciousintheMinmouseandnudemousexenograftmodelsofcoloncancer.ICG-001isapotentinhibitorofGBMstemcellsinculture.ICG001selectivelyinhibitsWnt/beta-catenin/CREBbindingprotein(CBP)signalingtoreversespulmonaryfibrosisandameliorateexperimentaldermalfibrosisinexperimentalmodels.ICG001iscurrentlyinclinicaltrialsforcoloncancerandleukemias.
Description:
CG001isasmallmoleculeinhibitorthattargetsWnt/β-cateninpathway.ItinhibitsTCF/β-cateninmediatedtranscriptionbycompetingwithβ-cateninforCBP(CREBbindingprotein)butnotp300bindingwithanIC50of3µM.ItcanbeusedtospecificallyevaluatetheroleofCBP/beta-cateninassociationonWNTsignalingandcellphysiology.
Synonym(s):
(6S,9aS)-N-benzyl-6-[(4-hydroxyphenyl)methyl]-8-(naphthalen-1-ylmethyl)-4,7-dioxo-3,6,9,9a-tetrahydro-2H-pyrazino[1,2-a]pyrimidine-1-carboxamide
Solubility:
SolubleinDMSO
Storage/StABIlity:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
1.EmamiKH,etal.Proc.Natl.Acad.Sci.USA2004Aug24;101(34):12682-7.
2.HendersonWRJr.,etal.Proc.Natl.Acad.Sci.USA2010Aug10;107(32):14309-14.
3.BeyerC,etal.AnnRheumDis.2013Jul;72(7):1255-8.
2.HendersonWRJr.,etal.Proc.Natl.Acad.Sci.USA2010Aug10;107(32):14309-14.
3.BeyerC,etal.AnnRheumDis.2013Jul;72(7):1255-8.
ScientificCategory:
WntSignaling
ProductType:
Inhibitor
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