YUM70 是一种选择性葡萄糖调节蛋白 78 抑制剂，抑制全长蛋白的 GRP78 ATPase 活性的IC50值为 1.5 μM。它在胰腺癌中诱导内质网应激介导的细胞凋亡。

YUM70 is a potent and selective glucose-regulated protein 78 (GRP78) inhibitor(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.

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.

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.

423145-35-1

C21H19ClN2O4

398.84

DMSO:100 mg/mL (250.73 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years