PROTAC-FAK-degrader-3-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

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PROTACFAKdegrader3

Cat.No.:HY-175459

分⼦式:C₄₈H₅₀N₈O₉

分⼦量:882.96

作⽤靶点:PROTACs;FAK

作⽤通路:PROTAC;ProteinTyrosineKinase/RTK

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PROTACFAKdegrader3是⼀种选择性的FAKPROTAC降解剂(DC50=1.08nM)。PROTACFAKdegrader3

诱导FAK降解依赖于泛素-蛋⽩酶体系统及其与FAK和CRBN的结合。PROTACFAKdegrader3通过对FAK⾮

催化活性的抑制上调MHC-I的基因转录和肿瘤细胞表⾯表达，进⽽导致抗原呈递增加和细胞毒性CD8T细胞

的激活。PROTACFAKdegrader3通过促进MHC-I表达和增强T细胞活化来增强体内抗肿瘤活性。PROTAC

FAKdegrader3可⽤于卵巢癌、肝细胞癌等靶向FAK降解的癌症研究。(粉⾊:FAK-IN-3:HY-143407，蓝⾊:

Thalidomide-4-OH:HY-103596，蓝⾊+⿊⾊:FAKligand-3:HY-W939883，⿊⾊：连接⼦)[1]。

IC50TargetCereblon

体外研究PROTACFAKdegrader3(CompoundD4)(0-1000nM,24h)inducesFAKdegradationinPA-1,ID8,4T1,

H22,HEY,MDA-MB-231,andPLC/PRF5cells,induces89%degradationofFAKat50nMand92%

degradationofFAKat500nMinPA-1cells[1].

PROTACFAKdegrader3(1μM)inhibitsFAK(99%)(IC50=0.44nM),STK33(92%),CLK4(87%),andFes

(86%)kinaseactivity[1].

PROTACFAKdegrader3(0.01-100μM,72h)exhibitsantiproliferativ