JI051是一种Hes1-PHB2相互作用稳定剂,能够与癌症相关蛋白伴侣prohibitin2(PHB2)相互作用,通过抑制Notch下游效应基因Hes1来诱导细胞周期停滞。具有抗肿瘤作用。
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JI051 is a stabilizer for the Hes1-PHB2 interaction, interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity[1].
JI051 causes G2/M cell-cycle arrest[1].JI051 (0.1-10 µM, 24 hours) significantly inhibits cell proliferation of HEK293 cells, with an EC50 of 0.3 μM[1]. Cell Proliferation Assay[1] Cell Line: HEK293 cells
[1]. Perron A, et al. Small-molecule screening yields a compound that inhibits the cancer-associated transcription factor Hes1 via the PHB2 chaperone. J Biol Chem. 2018 May 25;293(21):8285-8294.
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