YUM70 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.
MedKoo Cat#: 555922
Name: YUM70
CAS#: 423145-35-1
Chemical Formula: C21H19ClN2O4
Exact Mass: 398.1033
Molecular Weight: 398.84
Elemental Analysis: C, 63.24; H, 4.80; Cl, 8.89; N, 7.02; O, 16.05
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
To be determined | 0.0 | 0.00 |
The following data is based on the product molecular weight 398.84 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |