YUM70

• CAT Number: I038625
• CAS Number: 423145-35-1
• Molecular Formula: C21H19ClN2O4
• Molecular Weight: 398.843
• Purity: 98%
• Synonyms: YUM70; YUM-70; YUM 70
• Solubility: To be determined
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: N-[1,3-Benzodioxol-5-yl(5-chloro-8-hydroxy-7-quinolinyl)methyl]butanamide
• InChI: InChI=1S/C21H19ClN2O4/c1-2-4-18(25)24-19(12-6-7-16-17(9-12)28-11-27-16)14-10-15(22)13-5-3-8-23-20(13)21(14)26/h3,5-10,19,26H,2,4,11H2,1H3,(H,24,25)
• InChIKey: BIQMEYCMAGHOEQ-UHFFFAOYSA-N
• SMILES: CCCC(NC(C1=CC=C(OCO2)C2=C1)C3=CC(Cl)=C4C=CC=NC4=C3O)=O

YUM70 (Cat.No:I038625) is a potent inhibitor of GRP78 (Glucose-regulated protein, 78 kDa). YUM70, inhibited pancreatic cancer cell growth in vitro and showed in vivo efficacy in a pancreatic cancer xenograft model with no toxicity to normal tissues. YUM70 directly bound GRP78 and inactivated its function, resulting in ER stress-mediated apoptosis. A YUM70 analog conjugated with BODIPY show co-localization of the compound with GRP78 in the ER. Moreover, a YUM70-PROTAC (PROteolysis TArgeting Chimera) was synthesized to force degradation of GRP78 in pancreatic cancer cells. YUM70 showed a strong synergistic cytotoxicity with topotecan and vorinostat.

Reference

Samanta S, Yang S, Debnath B, Xue D, Kuang Y, Ramkumar K, Lee AS, Ljungman M, Neamati N. The hydroxyquinoline analog YUM70 inhibits GRP78 to induce ER stress-mediated apoptosis in pancreatic cancer. Cancer Res. 2021 Feb 2:canres.1540.2020. doi: 10.1158/0008-5472.CAN-20-1540. Epub ahead of print. PMID: 33531374.