dCDK9-202-生命科学试剂-MCE.pdfVIP

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Inhibitors•ScreeningLibraries•Proteins

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dCDK9-202

Cat.No.:HY-178861

分⼦式:C₄₀H₄₉N₇O₇S₂

分⼦量:803.99

作⽤靶点:PROTACs;CDK;Caspase;PARP;Apoptosis

作⽤通路:PROTAC;CellCycle/DNADamage;Apoptosis;Epigenetics

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性dCDK9-202是⼀种强效的CDK9PROTAC降解剂，其DC50值为3.5nM。dCDK9-202具有⼴谱抗肿瘤活性

，并能⼴泛破坏致癌转录组。dCDK9-202可激活Caspase-3/7，增加裂解型PARP的⽔平，并直接诱导肿瘤细

胞凋亡(apoptosis)。dCDK9-202能有效抑制TC-71肿瘤的⽣长，且在⼩⿏体内未观察到任何毒性反应。

dCDK9-202可⽤于研究EGFR驱动的癌症，例如⾁瘤(粉⾊：CDK9配体(HY-178862)；蓝⾊：CRBN配体(HY-

W248665)；⿊⾊：连接⼦(HY-N8015))[1]。

IC50TargetCDK9Caspase-3Caspase-7Cereblon

3.5nM(DC50)

体外研究dCDK9-202(10nM,0-24h)treatmentofTC-71cellswithin2hourscansignificantlyreducetheCDK9

proteinlevel,andcompleteandnearlycontinuousdegradationwasachievedwithin8hours[1].

dCDK9-202(0.1nM-1μM,24h)exhibitxnanomolarlevelsofproliferationinhibitoryactivityin12cancercell

linesderivedfromvarioustissuessuchaslung,liver,bone,andbrain.Forinstance,inTC-71