480073

Necrosulfonamide

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

• Szinonimák: 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
• Tapasztalati képlet (Hill-képlet): C₁₈H₁₅N₅O₆S₂
• CAS-szám: 432531-71-0
• Molekulatömeg: 461.47
• MDL-szám: MFCD02370191
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Terméknév: 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.
• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• Forma: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: dark yellow
• oldhatóság: DMSO: 100 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: 2-8°C
• SMILES string: [S](=O)(=O)(Nc3ncc[n+H]c3OC)c1ccc(cc1)\N=C(/[O-])\C=C\c2[s]c(cc2)[N+](=O)[O-]
• 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+
• Nemzetközi kémiai azonosító kulcs: FNPPHVLYVGMZMZ-XBXARRHUSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

Cell permeable: yes

Primary Target
human MLKL

Reversible: no

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

Use only fresh DMSO for reconstitution.

Egyéb megjegyzések

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

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable