Apoptosis-inducer-49-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

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Apoptosisinducer49

Cat.No.:HY-178940

分⼦式:C₃₆H₅₃N₃O₃

分⼦量:575.82

作⽤靶点:Apoptosis;CheckpointKinase(Chk);CDK;DNA/RNA

Synthesis;Bcl-2Family;Caspase

作⽤通路:Apoptosis;CellCycle/DNADamage

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Apoptosisinducer49是⼀种选择性细胞毒性药物，对CCRF-CEM⽩⾎病细胞具有⾼度特异性(IC50=2.68μ

M)，治疗指数(TI)为18.66。Apoptosisinducer49可诱导DNA损伤(γH2AX)和复制应激，激活Chk1-p21

通路，导致S期阻滞。Apoptosisinducer49通过线粒体途径(抑制Bcl-2和激活caspase-3)诱导CCRF-CEM

细胞凋亡(apoptosis)。Apoptosisinducer49可⽤于⽩⾎病的研究[1]。

体外研究Apoptosisinducer49(Compound16j)exhibitspotentcytotoxicityagainstCCRF-CEMcells(IC50=2.68μM),

showsnosignificantactivityagainstothercancercelllinesandnon-cancercelllines(IC5050μM),andthe

therapeuticindex(TI)is18.66[1].

Apoptosisinducer49(2.68-13.4μM,24h)demonstratesadose-dependentincreaseintheproportionof

apoptoticcellsandinducessignificantS-phasearrestinCCRF-CEMcells,whereat2.68μM,earlyapoptotic

(annexinV+/PI-)cellssignificantlyincreas