MKC8866 是一种选择性IRE1 RNase抑制剂，在体外的IC50为 0.29 μM，是水杨醛类似物。 它抑制乳腺癌细胞中的 IRE1 RNase，导致促肿瘤因子的产生减少，并且可以抑制前列腺癌 (PCa) 肿瘤的生长。它强烈抑制二硫苏糖醇诱导的 XBP1s 表达，EC50为 0.52 μM。

MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.

MKC8866 strongly suppresses DTT-induced X-box-binding protein 1-spliced (XBP1s) expression (EC50: 0.52?μM) and unstressed RPMI 8226 cells (IC50: 0.14?μM). MKC8866 (0.2-10 μM; 3 days) inhibits the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells, and MKC8866 (20 μM; 72?hours) is sufficient to completely block NSC 125973-induced expression of XBP1s [1]. MKC8866 (20?μM; 6 days) reduces the proliferation of all breast cancer cell lines and MKC8866 (20 μM; 48 hours) decreases the number of cells entering the S phase [2].

MKC8866 (oral ; 300 mg/kg; for 28 days) decreases tumor regrowth post-NSC 125973 withdrawal [1].

1338934-59-0

C18H19NO7

361.35

DMSO:16.67 mg/mL (46.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years