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商品描述
MW:445.4Da
CASRegistry#:328968-36-1
Formula:C24H19N3O6
Target:p300
Background:
C646bindstop300astheZ-isomerforminghydrogenbondsbetweenThr1411,tYR1467,Trp1466andArg1410onthesidechainsofp300andoxygenatomsofC646.C646isalsocapableofinhibitingavarietyofp300HATmutants,includingT1411A,Y1467F,W1466FandR1410AwithIC50valuesof3.4µM,7µM,5µMand2.5µMrespectively.
Description:
C646,apyrazolone-containingsmallmolecule,isacell-permeablehistoneacetyltransferase(HAT)inhibitorthatcompetitivelyandselectivelyinhibitstheHATactivityofp300,atranscriptionalco-activatorinvolvedinavarietyofgeneregulatorypathwaysandproteinacetylationevents,withtheKivalueof400nMandanIC50valueof1.6µM.
Synonym(s):
4-[(4Z)-4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoicacid
Solubility:
SolubleinDMSO
Storage/StABIlity:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
BowersEM,etal.ChemBiol.2010May28;17(5):471-82.
ScientificCategory:
HistoneAcetyltransferases
ProductType:
Inhibitor
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