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JI051

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Chemical Structure| 2234281-75-3 同义名 : -
CAS号 : 2234281-75-3
货号 : A1158758
分子式 : C22H24N2O3
纯度 : 98%
分子量 : 364.438
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(329.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Hes1 (helix-loop-helix transcription factor 1) is a downstream effector of Notch signaling and plays a crucial role in orchestrating developmental processes during the embryonic stage. Its aberrant signaling in adulthood is linked to the pathogenesis of cancer. JI051 can inhibitor Hes1 via cancer-associated protein chaperone PHB2 (prohibitin 2) and impair the ability of Hes1 to repress transcription. JI051 inhibited HEK293 cell proliferation with an EC50 of 0.3μM and induced cell-cycle arrest in G2/M at 1μM. Also it dose-dependently reduced cell growth of the human pancreatic cancer cell line MIA PaCa-2[2].
作用机制 JI051 inhibits Hes1 through binding to PHB2. It stabilizes PHB2’s interaction with Hes1 outside the nucleus.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.74mL

0.55mL

0.27mL

13.72mL

2.74mL

1.37mL

27.44mL

5.49mL

2.74mL
参考文献

[1]Perron A, Nishikawa Y, 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.

[2]Perron A, Nishikawa Y, Iwata J, Shimojo H, Takaya J, Kobayashi K, Imayoshi I, Mbenza NM, Takenoya M, Kageyama R, Kodama Y, Uesugi M. 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. doi: 10.1074/jbc.RA118.002316. Epub 2018 Mar 9. PMID: 29523683; PMCID: PMC5971435.