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公司地址
苏州工业园区生物纳米园A4#216
联系电话
4000-520-616 / 18915418616
传真号码
0512-67156496
电子邮箱
info@ebiomall.com
公司网址
https://www.ebiomall.com
商品描述
MW:448.54Da
Formula:C24H24N4O3S
Background:
Tankyrase1andtankyrase2aremembersofPARPfamily.TheycanuseNAD+assubstratestotransferADP-ribosepolymersontotargetproteins.ThetankyrasesbindandPARSylateaxinproteinswhicharethenegativeregulatorofWntpathway.Thustankyrasesarepromisingtargetsfortreatmentforadenomatouspolyposiscoli.Tankyraseinhibitor49isanoptimizationoftheprevioushitcompoundinhibitor8withimprovedpotencyandselectivity.Ithasexcellenteffectsinbothtankyraseassayandcellularassay(totalβ-catenindegradationassayinSW480cells)withIC50valuesof0.1nMand1.9nM,respectively.Inaddition,itisfoundtobeadualbinderwithboththenicotinamidepocketandtheinducedpocketoftheenzymes.Intheinvivostudiesinrodents,tankyraseinhibitor49isfoundtopotentlyinhibitTNKS2autoparsylationwithIC50=7.6nM.ItalsocausesstABIlizationandaccumulationofaxinproteininSW480cellswithEC50=4nM.InDLD-1cellswithtruncatedAPC,theinhibitorinhibitstheSTFreportertranscriptionwithIC50=0.3nM,suggestingitsdownstreaminhibitoryactivityonWnt-associatedtranscription.
Description:
TankyraseInhibitor49(TNKSi49)isapotent,selectiveandorallybioavailableinhibitoroftankyrasewithIC50valueof0.1nM.
Synonym(s):
N-((1r,4r)-4-(4-cyanophenoxy)cyclohexyl)-3-((4-oxo-3,4-dihydroquinazolin-2-yl)thio)propanamide
Purity:
≥98%byHPLC
Storage/Stability:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
HuaZ,etal.J.Med.Chem.2013,56(24):10003-10015.
ScientificCategory:
PARPInhibitor
ProductType:
Inhibitor
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