480073

Necrosulfonamide

≥95% (HPLC), solid, MLKL inhibitor, Calbiochem^®

• 別名: MLKL Inhibitor, Necrosulfonamide, Necrosis Inhibitor III, Mixed Lineage Kinase Domain-Like Protein Inhibitor, Necrosome Inhibitor II, Necrosulfonamide, (E)-N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide
• 実験式（ヒル表記法）: C₁₈H₁₅N₅O₆S₂
• CAS番号: 432531-71-0
• 分子量: 461.47
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 製品名: MLKL Inhibitor, Necrosulfonamide, MLKL Inhibitor, Necrosulfonamide, CAS 432531-71-0, is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function.
• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: dark yellow
• 溶解性: DMSO: 100 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• InChI: 1S/C18H15N5O6S2/c1-29-18-17(19-10-11-20-18)22-31(27,28)14-6-2-12(3-7-14)21-15(24)8-4-13-5-9-16(30-13)23(25)26/h2-11H,1H3,(H,19,22)(H,21,24)/b8-4+
• InChI Key: FNPPHVLYVGMZMZ-XBXARRHUSA-N

詳細

詳細

A cell-permeable acrylamide compound that inhibits human, but not murine, MLKL adaptor function via covalent modification of Cys86 and is more potent than Nec-1 (Cat. No. 480065) in preventing necrotic/necroptotic death in human HT-29 (IC₅₀ = 124 nM and 2 µM, respectively), being ineffective against necrosis/necroptosis in murine L929 or apoptosis in human RIP3-null Panc-1 cells. Unlike Nec-1, which prevents necrosome formation by blocking RIP1-RIP3 interaction, MLKL prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with further downstream effectors.

A cell-permeable acrylamide compound that inhibits human, but not murine, MLKL adaptor function via covalent modification of Cys86 through Michael addition and is more potent than the RIP1 inhibitor Nec-1 (Cat. No. 480065) in preventing necrotic/necroptotic death in human HT-29 (IC₅₀ = 124 nM and 2 µM with respective drug against 20 ng/mL TNF-&alpha/100 nM Smac mimetic/20 µM Z-VAD-induced death) and FADD-null Jurkat cultures (80% protection against 200 ng/mL TNF-&alpha-induced death by 0.5 µM NSA or 10 µM Nec-1), being ineffective against blocking necrosis/necroptosis in murine L929 or apoptosis in human RIP3-null Panc-1 cells even at concentrations as high as 5 µM. Unlike Nec-1, which prevents necrosome formation by blocking RIP1-RIP3 interaction, MLKL prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with further downstream effectors.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
human MLKL

Reversible: no

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Use only fresh DMSO for reconstitution.

その他情報

Dunai, Z.A., et al. 2012. PLoS One7, e41945.
Sun, L., et al. 2012. Cell 148, 213.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable