For research use only. Not for therapeutic Use.
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.
| Catalog Number | I038625 |
| CAS Number | 423145-35-1 |
| Synonyms | YUM70; YUM-70; YUM 70; |
| Molecular Formula | C21H19ClN2O4 |
| Purity | 98% |
| Solubility | To be determined |
| Appearance | Solid powder |
| 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-hydroxyquinolin-7-yl)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(=O)NC(C1=CC2=C(C=C1)OCO2)C3=CC(=C4C=CC=NC4=C3O)Cl |
| 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. |
