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商品描述
MW:312.4Da
CASRegistry#:935881-37-1
Formula:C18H20N2O3
Target:HDAC
Background:
AR-42induceshistoneH3acetylation,α-tubulinacetylationandp21up-regulation,whichhavebeenconsideredasthehallmarkindicatorsofHDACinhibition.AR-42hasbeenfoundtomodulateseveralapoptosisinhibitorsaswellascellsurvivalregulator,includingAkt,Bcl-xL,Bax,Ku70andsurviving,andexertpotentantitumoractivityagainstmultipletumortypes,suchashumanprostateandhepaticcancers,atleastpartiallythroughPI3K/Aktpathwayinhibition.AR-42hasbeendesignatedanorphandrugbytheFDAforthetreatmentofmeningiomaandschwannomaofthecentralnervoussystem.Meningiomaandschwannomaarerare,benigntumorsthatcanpresentindifferentlocationswithinthebrainandthespinalcordandmaycausesubstantialmorbidity.
Description:
AR-42(alsoknownasOSU-HDAC42),aderivativeofhydroxamate-tetheredphenylbutyrateisabroad-spectrumdeacetylaseinhibitorofbothhistoneandnon-histoneproteins.AR-42treatmentinduceshistonehyperacetylationandp21WAF/CIP1overexpression,inhibitsgp130/Stat3pathwayandinducesapoptosisandcellcyclearrestinmultiplemyelomacells.
Synonym(s):
OSU-HDAC42;N-hydroxy-4-[[(2S)-3-methyl-2-phenylbutanoyl]amino]benzamide
Purity:
≥99%byHPLC
BIOLOGicalActivity:
AR-42isapan-HDACinhibitorwithIC50of16-30nM.Ithasdemonstratedgreaterpotencyandactivityinsolidtumorsandhematologicalmalignancies(includingchroniclymphocyteleukemia,orCLL,B-celllymphoma,prostateandovariancancers)whencomparedtovorinostat(SAHA),thefirstoftwomarketedcompoundintheclass.
Solubility:
SolubleinDMSO
Storage/StABIlity:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
1.Burns,S.S.,etal.CancerRes.2013Jan15;73(2):792-803.
2.Zhang,S.,etal.IntJCancer.2011Jul1;129(1):204-13.
3.Lucas,D.M.,etal.PLoSOne.2010Jun3;5(6):e10941
2.Zhang,S.,etal.IntJCancer.2011Jul1;129(1):204-13.
3.Lucas,D.M.,etal.PLoSOne.2010Jun3;5(6):e10941
ScientificCategory:
DeacetylaseInhibitor
ProductType:
Inhibitor
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