WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555922
Description: 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
Chemical Formula: C21H19ClN2O4
Exact Mass: 398.1033
Molecular Weight: 398.843
Elemental Analysis: C, 63.24; H, 4.80; Cl, 8.89; N, 7.02; O, 16.05
Synonym: YUM70; YUM-70; YUM 70;
IUPAC/Chemical Name: N-[1,3-Benzodioxol-5-yl(5-chloro-8-hydroxy-7-quinolinyl)methyl]butanamide
InChi Key: BIQMEYCMAGHOEQ-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: CCCC(NC(C1=CC=C(OCO2)C2=C1)C3=CC(Cl)=C4C=CC=NC4=C3O)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: to be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 398.843 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|
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.
GRP78 (Glucose-regulated protein, 78 kDa) is a key regulator of ER (endoplasmic reticulum) stress signaling. Cancer cells are highly proliferative and have high demand for protein synthesis and folding, which results in significant stress on the ER. To respond to ER stress and maintain cellular homeostasis, cells activate the unfolded protein response (UPR) that promotes either survival or apoptotic death. Cancer cells utilize the UPR to promote survival and growth