WntHedgehogNotch Pathway抑制剂整理版

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1、WntinhibitorsICG-001M.Wt:548.63Formula:C33H32N4O4Solubility:DMSO≥110mg/mLWater<1mg/mLEthanol≥45mg/mLPurity:>99%Storage:at-20℃2yearsCASNo.:780757-88-2BiologicalActivityICG-001isaselectiveWnt/β-cateninsignallinginhibitorwithanIC50of3μM.AfterselectivelybindingofICG-001totheNH2terminusof

2、cyclicAMPresponseelementbindingprotein(CREB),ICG-001preventedbeta-catenin/TCFsignaling.ICG-001elevatedtheactivitiesofcaspaseincoloncarcinomacelllines,butnotnormalcellsviadownregulationofsurvivin.ItisexhibitedthatICG-001rescuesdefectsinneuronaldifferentiationandreversepulmonaryfibrosi

3、s.ICG-001alsosuppressedtheinteractionbetweenCREBandγ-catenin.[1]ICG-001selectivelyinducesapoptosisintransformedcellsbutnotinnormalcoloncells.AndICG-001reducesinvitrogrowthofcoloncarcinomacells.ICG-001efficaciouslytreatedthecoloncancerintheMinmouseandnudemousexenograftmodels.XAV939M.W

4、t:312.31Formula:C14H11F3N2OSSolubility:DMSO≥3mg/mLWater<1mg/mLEthanol≥5mg/mLPurity:>99%Storage:at-20℃2yearsCASNo.:284028-89-3BiologicalActivityXAV939isasmallmoleculeandselectiveWntpathwaytranscriptionfactorβ-catenin-mediatedtranscriptioninhibitorandaxinstabilizingagentwithIC50of11and

5、4nMfortheinhibitionofTNKS1andTNKS2,respectively.Itstimulatesbeta-catenindegradationbystabilizingaxin,theconcentration-limitingcomponentofthedestructioncomplexandstabilizesaxinbyinhibitingthepoly-ADP-ribosylatingenzymestankyrase1andtankyrase2.Bothtankyraseisoformsinteractwithahighlyco

6、nserveddomainofaxinandstimulateitsdegradationthroughtheubiquitin-proteasomepathway.DeregulatedWnt/b-cateninpathwayactivityhasbeenimplicatedinmanycancers.HedgehoginhibitorsCyclopamineM.Wt:411.62Formula:C27H41NO2Solubility:DMSO≥6mg/mLWater<1mg/mLEthanol≥39mg/mLPurity:>99%Storage:at-20℃

7、2yearsCASNo.:4449-51-8BiologicalActivityCyclopamineinhibitsthehedgehogsignalingpathway(Hh)byinfluencingthebalancebetweentheactiveandinactiveformsoftheSmoothenedprotein.Thehedgehogsignalingpathwaycarriesoutimportantfunctionsinembryonicdevelopmentandwhenitgoesawry,deformitiescanoccur.H

8、owever,erran