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Sulindac

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Chemical Structure| 38194-50-2 同义名 : MK-231
CAS号 : 38194-50-2
货号 : A253022
分子式 : C20H17FO3S
纯度 : 98%
分子量 : 356.411
MDL号 : MFCD00599589
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(140.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • COX
描述 Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2. Treatment with sulindac not only inhibited tumor formation but decreased small bowel Cox-2 and prostaglandin E(2) to baseline and restored normal levels of apoptosis[3]. Sulindac (0.1 mM to 0.5 mM) causes limited death in both p53 wt and p53 null HCT116 cells, but in combination with vitamin C, it dramatically increases almost 5-fold in cell death in p53 wt HCT116 cells relative to the vitamin C alone, and such an effect is involving caspase activation and p53 function in these cells, and via ROS-mediated pathway. Sulindac combined with vitamin C significantly increases PUMA levels, but shows no effect on Bim, Bcl-2 and Mcl-1 levels[4]. Moreover, celecoxib and sulindac can inhibit TGF-β1-induced EMT (epithelial-mesenchymal transition) and suppress lung cancer cell migration and invasion via downregulation of SIRT1(class III deacetylase sirtuin 1) [5]. Sulindac can protect normal astrocytes against oxidative stress. Sulindac induces differentiation of both NSC ( neural stem cells) and GSC (glioblastoma stem cells) cells and sulindac upregulates neurogenesis in NSC. The differentiated NSC are also protected from oxidative stress damage, whereas the differentiation of GSC by sulindac increases the sensitivity of these cells to agents that cause oxidative stress[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00275756 Glaucoma Not Applicable Withdrawn - Austria ... 展开 >> Department of Clinical Pharmacology Vienna, Austria, A-1090 收起 <<
NCT00283803 - Completed - -
NCT02003703 Hepatitis B H... 展开 >>IV 收起 << Phase 3 Recruiting - Chile ... 展开 >> Hospital Gustavo Fricke Recruiting Viña del Mar, Valparaíso, Chile Contact: Jose I Vargas, MD    62473415 ext +56 9    jivargasd@icloud.com    Contact: Daniela Jensen, MD    62473409 ext +56 9    daniela_jensen@hotmail.com    Principal Investigator: Jose I Vargas, MD          Principal Investigator: Daniela Jensen, MD          Principal Investigator: Francisco Fuster, MD          Principal Investigator: Valeska Sarmiento 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL
参考文献

[1]Yamamoto Y, Yin MJ, et al. Sulindac inhibits activation of the NF-kappaB pathway. J Biol Chem. 1999 Sep 17;274(38):27307-14.

[2]Piazza GA, Rahm AL, et al. Antineoplastic drugs sulindac sulfide and sulfone inhibit cell growth by inducing apoptosis. Cancer Res. 1995 Jul 15;55(14):3110-6.

[3]Boolbol SK, Dannenberg AJ, Chadburn A, et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res. 1996;56(11):2556-2560

[4]Gong EY, Shin YJ, Hwang IY, et al. Combined treatment with vitamin C and sulindac synergistically induces p53- and ROS-dependent apoptosis in human colon cancer cells. Toxicol Lett. 2016;258:126-133

[5]Cha BK, Kim YS, Hwang KE, et al. Celecoxib and sulindac inhibit TGF-β1-induced epithelial-mesenchymal transition and suppress lung cancer migration and invasion via downregulation of sirtuin 1. Oncotarget. 2016;7(35):57213-5722

[6]Allani SK, Weissbach H, Lopez Toledano MA. Sulindac induces differentiation of glioblastoma stem cells making them more sensitive to oxidative stress. Neoplasma. 2018;65(3):376-388