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YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. It induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 38 € | In Stock | |
5 mg | 83 € | In Stock | |
10 mg | 130 € | In Stock | |
25 mg | 264 € | In Stock | |
50 mg | 389 € | In Stock | |
100 mg | 553 € | In Stock | |
200 mg | 749 € | In Stock | |
1 mL x 10 mM (in DMSO) | 92 € | In Stock |
Description | YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. It induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. |
Targets&IC50 | GRP78:1.5 μM |
In vitro | YUM70, inhibited pancreatic cancer cell growth in vitro.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. |
In vivo | YUM70 in vivo efficacy in a pancreatic cancer xenograft model with no toxicity to normal tissues.YUM70 is a novel inducer of ER stress with preclinical efficacy as a monotherapy or in combination with topoisomerase and HDAC inhibitors in pancreatic cancer. |
Molecular Weight | 398.84 |
Formula | C21H19ClN2O4 |
Cas No. | 423145-35-1 |
Smiles | CCCC(=O)NC(c1ccc2OCOc2c1)c1cc(Cl)c2cccnc2c1O |
Relative Density. | 1.373 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (250.73 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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