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文件名称:HDAC-IN-27-dihydrochloride-生命科学试剂-MCE.pdf
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文档摘要

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Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

HDAC-IN-27dihydrochloride

Cat.No.:HY-142690A

CASNo.:3069831-25-7

分?式:C??H??Cl?N?O?

分?量:423.34

作?靶点:Apoptosis;HDAC

作?通路:Apoptosis;CellCycle/DNADamage;Epigenetics

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性HDAC-IN-27dihydrochloride(Compound11h)是?种有效的、具有?服活性的HDACI类选择性抑制剂,对

HDAC1-3的IC50值范围为0.43?3.01nM。HDAC-IN-27dihydrochloride还具有体内和体外抗癌活性。

HDAC-IN-27对急性髓系??病(AML)细胞系表现出显著的抗增殖活性,并通过诱导细胞凋亡(apoptosis)和

组蛋??酰化(AcHH3和AcHH4)发挥作?。HDAC-IN-27dihydrochloride可以?于急性髓系??病(AML)的

研究[1]。

IC50TargetHDAC1HDAC2HDAC3

3.01nM(IC50)18.54nM(IC50)0.435nM(IC50)

体外研究Inwt-p53MV4-11cells,HDAC-IN-27dihydrochloride(11h)leadstopro-caspase-3cleavage,apparent

apoptoticcelldeath,andaccumulationofsub-G1cellpopulationwhileinducingG2/MarrestinHL60cells