Sulindac Sulfide - CAS 32004-67-4 - Calbiochem

别名

Sulindac Sulfide - CAS 32004-67-4 - Calbiochem,(Z)-5-Fluoro-2-methyl-1-[ p-(methylthio)benzylidene]indene-3-acetic Acid

一般描述

A cell-permeable, active metabolite of Sulindac (Cat. No. 574100). Strongly inhibits Ras-induced malignant transformation and Ras/Raf-dependent transactivation. Also decreases the Ras-induced activation of c-Raf-1 kinase. Inhibits growth and induces apoptosis in prostate cancer cell lines. Selectively inhibits COX-1 (ID50 = 500 nM) compared to prostaglandin H synthase-2 (PGHS-2; COX-2; ID50 = 14 µM). Preferentially inhibits the secretion of Aβ42 in CHO cells stably transfected with both APP75, and the PS1 mutant M146L. An active metabolite of the non-steroidal anti-inflammatory drug Sulindac (Cat. No. 574100). Inhibits Ras signaling. Strongly inhibits Ras-induced malignant transformation and Ras/Raf-dependent transactivation. Also decreases the Ras-induced activation of c-Raf-1 kinase. Inhibits cell growth and induces apoptosis in a time-and dose-dependent manner. Selectively inhibits prostaglandin H synthase-1 (PGHS-1; COX-1; ID50 = 0.5 µM) relative to prostaglandin H synthase-2 (PGHS-2; COX-2; ID50 = 14 µM). Reduces Aβ42 production independently of COX inhibition.

生化/生理作用

Cell permeable: yes ID50 = 500 nM against COX-1 Product does not compete with ATP. Reversible: no

其他说明

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Meade, E.A., et al. 1993. J. Biol. Chem. 268, 6610.