CDC20-HSP90-IN-1-生命科学试剂-MCE.pdfVIP

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CDC20/HSP90-IN-1

Cat.No.:HY-179012

分⼦式:C₃₃H₃₆Cl₄N₁₂O₅

分⼦量:822.53

作⽤靶点:APC;CDK;Raf;Akt;HSP

作⽤通路:CellCycle/DNADamage;MAPK/ERKPathway;

PI3K/Akt/mTOR;MetabolicEnzyme/Protease

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性CDC20/HSP90-IN-1(Compound2b)是⼀种Cdc20/Hsp90抑制剂，对Cdc20的Kd值为16.2μM，对Hsp90

α的Kd值为0.241μM。CDC20/HSP90-IN-1通过降低p53介导的Cdc20表达、上调Bim表达、下调Cyclin

B1表达以及通过破坏Hsp90分⼦伴侣功能⼲扰B-Raf和AKT通路，从⽽发挥强⼤的抗肿瘤活性。

CDC20/HSP90-IN-1克服了Vemurafenib(HY-12057)诱导的耐受⿊⾊素瘤[1]。

IC50TargetCDK1/cyclinB1B-RafHSP90α

0.241μM(Kd)

REFERENCES

[1].ChenQ,etal.DiscoveryofCdc20/Hsp90Dual-TargetInhibitorswithPotentAntitumorActivityforTherapyofAcquiredResistant

Melanoma.JMedChem.2025Nov13;68(21):22428-22454.

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