JI130

• CAT Number: I029787
• CAS Number: 2234271-86-2
• Molecular Formula: C23H24N2O3
• Molecular Weight: 376.45
• Purity: ≥95%
• Synonyms: (E)-3-(7-methoxy-1H-indol-3-yl)-N-[2-(2-prop-2-enoxyphenyl)ethyl]prop-2-enamide
• InChI: InChI=1S/C23H24N2O3/c1-3-15-28-20-9-5-4-7-17(20)13-14-24-22(26)12-11-18-16-25-23-19(18)8-6-10-21(23)27-2/h3-12,16,25H,1,13-15H2,2H3,(H,24,26)/b12-11+
• InChIKey: BNTYDBBGNPFECO-VAWYXSNFSA-N
• SMILES: COC1=CC=CC2=C1NC=C2C=CC(=O)NCCC3=CC=CC=C3OCC=C

JI130(CAT: I029787), a derivative of JI051, is a small-molecule stabilizer of the Hes1–PHB2 (prohibitin 2) protein–protein interaction. It functions by inhibiting the repressive activity of Hes1 on transcription, thereby modulating downstream gene expression pathways involved in cell proliferation and differentiation. JI130 has shown promising anti-tumor activity, significantly reducing tumor growth in a murine pancreatic cancer model, suggesting its potential as a novel therapeutic candidate for managing pancreatic cancer. By targeting transcriptional regulation mechanisms, JI130 offers a unique approach for cancer research and drug development focused on Notch signaling and transcription factor modulation.

Reference

[1]. Amelie Perron, 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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