574102

Sulindac Sulfide

A cell-permeable, active metabolite of Sulindac.

• 別名: Sulindac Sulfide, (Z)-5-Fluoro-2-methyl-1-[ p-(methylthio)benzylidene]indene-3-acetic Acid
• 実験式（ヒル表記法）: C₂₀H₁₇FO₂S
• CAS番号: 32004-67-4
• 分子量: 340.41
• MDL番号: MFCD00869764
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (TLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: yellow-orange
• 溶解性: DMSO: 25 mg/mL; ethanol: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 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 Key: LFWHFZJPXXOYNR-RQZCQDPDSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

ID50 = 500 nM against COX-1

Product does not compete with ATP.

Reversible: no

警告

Toxicity: Harmful & Carcinogenic / Teratogenic (E)

その他情報

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.

法的情報

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

安全性情報

• ピクトグラム: GHS08,GHS07
• シグナルワード: Danger
• 危険有害性情報: H302,H317,H334,H361
• 注意書き: P202 - P261 - P280 - P301 + P312 - P302 + P352 - P308 + P313
• 危険有害性の分類: Acute Tox. 4 Oral - Repr. 2 - Resp. Sens. 1 - Skin Sens. 1
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable