574102

Sulindac Sulfide

A cell-permeable, active metabolite of Sulindac.

• 同義詞: Sulindac Sulfide, (Z)-5-Fluoro-2-methyl-1-[ p-(methylthio)benzylidene]indene-3-acetic Acid
• 經驗公式（希爾表示法）: C₂₀H₁₇FO₂S
• CAS號碼: 32004-67-4
• 分子量：: 340.41
• MDL號碼: MFCD00869764
• 分類程式碼代碼: 51111800
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (TLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze
• 顏色: yellow-orange
• 溶解度: DMSO: 25 mg/mL; ethanol: 5 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 10-30°C
• InChI: 1S/C20H17FO2S/c1-12-17(9-13-3-6-15(24-2)7-4-13)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9+
• InChI 密鑰: LFWHFZJPXXOYNR-RQZCQDPDSA-N

描述

一般說明

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

警告

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

其他說明

Weggen, S., et al. 2001. Nature414, 212.
Lim, J.T., et al. 1999. Biochem. Pharmacol. 58, 1097.
Herrmann, C., et al. 1998. Oncogene 17, 1769.
Picariello, L., et al. 1998. Eur. J. Pharmacol. 360, 105.
Arber, N., et al. 1997. Gastroenterology 113, 1892.
Meade, E.A., et al. 1993. J. Biol. Chem. 268, 6610.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 象形圖: GHS08,GHS07
• 訊號詞: Danger
• 危險聲明: H302,H317,H334,H361
• 防範說明: P202 - P261 - P280 - P301 + P312 - P302 + P352 - P308 + P313
• 危險分類: Acute Tox. 4 Oral - Repr. 2 - Resp. Sens. 1 - Skin Sens. 1
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable