HEMTAC-WEE1-degrader-1-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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HEMTACWEE1degrader-1

Cat.No.:HY-173320

CASNo.:3002417-64-0

分⼦式:C₅₇H₇₁N₁₅O₆

分⼦量:1062.27

作⽤靶点:Wee1;HSP

作⽤通路:CellCycle/DNADamage;MetabolicEnzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性HEMTACWEE1degrader-1是⼀种WEE1的HSP90介导靶向嵌合体(HEMTAC)降解剂(HSP90酶抑制活性为

IC50:16.76nM)。HEMTACWEE1degrader-1能促进WEE1的泛素化和降解。HEMTACWEE1degrader-1可

阻断G2/M细胞周期。HEMTACWEE1degrader-1在急性髓系⽩⾎病(AML)患者来源的异种移植(PDX)模型中

具有抗癌活性。HEMTACWEE1degrader-1可⽤于AML的研究。(粉⾊：HSP90结合剂；蓝⾊：WEE1配体

；⿊⾊：连接⼦)。

IC50TargetHSP90

16.76nM(IC50)

体外研究HEMTACWEE1degrader-1(Compound9c)(72h)inhibitstheproliferationactivityofMV-4-11cells(IC50:

8.08nM)andprimaryAMLcells(IC50:4.77nM)[1].

HEMTACWEE1degrader-1(0.01-10μM,12h)degradesWEE1proteininMV-4-11cellsandhasaminor

effectonAKTprotein,indicatingthatthiseffectisindependentofHSP90inhibition[1].

HEMTACWEE1degrader-1(0.1-10μM,12h)promotestheexpressionofWEE1mRNAinMV-4-11cellsin

aconcentration-dependentmanner[1].

HEMT