DPP9-IN-2-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

DPP9-IN-2

Cat.No.:HY-179348

CASNo.:3020859-44-0

分⼦式:C₃₃H₃₃F₂N₃O₂

分⼦量:541.63

作⽤靶点:DipeptidylPeptidase;HIV;Pyroptosis

作⽤通路:MetabolicEnzyme/Protease;Anti-infection;Apoptosis;

Immunology/Inflammation

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性DPP9-IN-2是⼀种选择性、强效的且具有⼝服活性的⼆肽基肽酶9(DPP9)抑制剂,IC50值为12.9nM。DPP9-

IN-2对DPP8的选择性指数为59,且对包括DPP2、DPP4、FAP和PREP在内的相关肽酶⽆显著抑制活性。

DPP9-IN-2可诱导癌细胞焦亡(pyroptosis),与⾮核苷类逆转录酶抑制剂联⽤时具有较弱的抗HIV-1协同活性

。DPP9-IN-2可⽤于癌症和感染的研究。

IC50TargetDPP-9HIV-1

12.9nM(IC50)

体外研究DPP9-IN-2(Compound6e)(0.05-5μM;24-48h)inducespyroptosisinTHP-1cells,promotingLDHrelease

andSYTOXGreenuptake[1].

DPP9-IN-2(0.5-5μM;24h)inducespyroptosisdependingonDPP9,CASP1,andGSDMD,andpyroptosisis

significantlyinhibitedordelayedinDPP9-knockdown,CASP1-KO,orGSDMD-KOTHP-1cells[1].

DPP9-IN-2(5μM)showsweaksynergisticanti-HIV-1activitywhencombinedwithnon-nucleosidereverse

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