Sulindac 是一种非甾体类抗炎剂，可抑制COX-2的活性，也可抑制 COX-2 的过表达。它是一种亚磺酰基茚衍生物前药，具有潜在的抗肿瘤活性。

Sulindac is a sulfinylindene derivative prodrug with potential antineoplastic activity. Converted in vivo to an active metabolite, sulindac, a nonsteroidal anti-inflammatory drug (NSAID), blocks cyclic guanosine monophosphate-phosphodiesterase (cGMP-PDE), an enzyme that inhibits the normal apoptosis signal pathway; this inhibition permits the apoptotic signal pathway to proceed unopposed, resulting in apoptotic cell death.

Min/+小鼠肠组织中,Sulindac不改变PGE 2和LTB 4的水平,但减少肿瘤数量.在鼠modelof家族性腺瘤性息肉模型中,Sulindac降低小肠COX-2和前列腺素E（2）,抑制肿瘤形成.

在结肠癌细胞系中,Sulindac和其代谢物硫化舒林酸和磺基舒林能抑制NF-κB途径,降低由于Sulindac介导的IKKbeta激酶活性。HT-29细胞中,Sulindac明显降低细胞生长数量。在多种上皮细胞和成纤维细胞的肿瘤细胞系中,Sulindac能够抑制细胞生长。在CRC细胞系DLD1和SW480中,Sulindac抑制 beta-catenin/TCF介导的基因转录,并降低非磷酸化的beta-catenin的水平。

38194-50-2

C20H17FO3S

356.41

MK-231;舒林酸;Sulindac sulfoxide;Clinoril;Arthrocine

Ethanol:9 mg/mL (25.25 mM)
DMSO:66 mg/mL (185.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years