P-gp-inhibitor-30-生命科学试剂-MCE.pdfVIP

Hotline:400-820-3792

Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

P-gpinhibitor30

Cat.No.:HY-178349

分⼦式:C₂₂H₁₅FN₄O₂

分⼦量:386.38

作⽤靶点:P-glycoprotein;Apoptosis;Autophagy

作⽤通路:MembraneTransporter/IonChannel;Apoptosis;Autophagy

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性P-gpinhibitor30是⼀种强效的P-gp抑制剂，能逆转乳腺癌的多药耐药性，使耐药细胞对Doxorubicin

(ADM)(HY-15142)敏感。P-gpinhibitor30与ADM联合使⽤时，可促进耐药乳腺癌细胞细胞凋亡(

apoptosis)，诱导⾃噬(autophagy)，抑制细胞增殖、迁移和侵袭。P-gpinhibitor30在体外和体内均能抑制

乳腺癌肿瘤⽣长。P-gpinhibitor30可⽤于耐药性乳腺癌的相关研究[1]。

体外研究P-gpinhibitor30(compoundA38)(0.1μM)reversesADMresistanceinMDA-MB-231/ADMcells,potently

reducingtheIC50ofADMfrom785.46μMto2.05μM[1].

P-gpinhibitor30(0.125-4μM)significantlyinhibitsP-gpATPaseactivityatdifferentconcentrationsina

concentration-dependentmanner[1].

P-gpinhibitor30interactswithP-gptoinhibititsfunctionwithoutdownregulatingitsexpression,and

stabilizestheprotein,therebyreducingitsdegradationinMCF7/ADMcellsuponincreasingtemperature[1].

P-gpinhibitor30(6h)significantlyincreasesRh123intensityinMCF7/ADMcellsand