480073

Necrosulfonamide

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

• Synonim(y): Necrosis Inhibitor III, Mixed Lineage Kinase Domain-Like Protein Inhibitor, Necrosome Inhibitor II, Necrosulfonamide,(E)-N-(4-(N-(3-metoksypirazyno-2-ylo)sulfamoilo)fenylo)-3-(5-nitrotiofeno-2-ylo)akryloamid
• Wzór empiryczny (zapis Hilla): C₁₈H₁₅N₅O₆S₂
• Numer CAS: 432531-71-0
• Masa cząsteczkowa: 461.47
• Numer MDL: MFCD02370191
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Nazwa produktu: 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.
• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: dark yellow
• rozpuszczalność: DMSO: 100 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• ciąg SMILES: [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+
• Klucz InChI: FNPPHVLYVGMZMZ-XBXARRHUSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
human MLKL

Reversible: no

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Use only fresh DMSO for reconstitution.

Inne uwagi

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

Informacje prawne

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

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable