YUM70 |
| カタログ番号GC62388 |
YUM70 は、グルコース調節タンパク質 78 (GRP78) の強力かつ選択的な阻害剤であり、全長タンパク質の GRP78 ATPase 活性を阻害する IC50 は 1.5 μM です。 YUM70 は、膵臓癌の小胞体 (ER) ストレスを介したアポトーシスを誘導します。 YUM70 は、膵臓癌異種移植モデルにおいても in vivo で有効です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 423145-35-1
Sample solution is provided at 25 µL, 10mM.
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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. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model[1].
YUM70 shows selective cytotoxicity for MIA PaCa-2, PANC-1, BxPC-3 cells (IC50=2.8, 4.5, and 9.6 μM, respectively) over normal pancreatic tissue-derived HPNE cells (IC50>30 μM)[1].YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells[1].
YUM70 (30 mg/kg; i.p. 5 days a week for 7 weeks) inhibits tumor growth in a MIA PaCa-2 xenograft model[1].YUM70 (15 mg/kg; i.v.) exhibits t1/2 (1.40 h), CL (724.04 mL/h/kg), and Vss (1162.73 mL/kg) in mice[1].YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t1/2 (2.74 h), and CL (9230.15 mL/h/kg) in mice[1].
[1]. Samanta S, et, al. The hydroxyquinoline analog YUM70 inhibits GRP78 to induce ER stress-mediated apoptosis in pancreatic cancer. Cancer Res. 2021 Feb 2;canres.1540.2020.
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