480065

Necrostatin-1

≥95% (HPLC), crystalline solid, necroptosis inhibitor, Calbiochem

• Szinonimák: Necrostatin-1, Nec-1, Necrosome Inhibitor I, 5-(Indol-3-ylmethyl)-(2-thio-3-methyl)hydantoin, Necrosis Inhibitor II, Methyl-thiohydantoin-tryptophan, MTH-Trp, Receptor-Interacting Protein 1 Inhibitor I, RIPK 1 Inhibitor I, Nec1, RIP1 Inhibitor I
• Tapasztalati képlet (Hill-képlet): C₁₃H₁₃N₃OS
• CAS-szám: 4311-88-0
• Molekulatömeg: 259.33
• MDL-szám: MFCD00056916
• UNSPSC kód: 12352200
• NACRES: NA.77

Tulajdonságok

• Terméknév: Necrostatin-1, Necrostatin-1, CAS 4311-88-0, is a cell-permeable, potent, and selective blocker of necroptosis (EC₅₀ = 494 nM in FADD-deficient Jurkat cells treated with TNF-α).
• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• Forma: crystalline solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: yellow
• oldhatóság: DMSO: 10 mg/mL; methanol: 5 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: 2-8°C
• SMILES string: S=C1NC(C(=O)N1C)Cc2c3c([nH]c2)cccc3
• InChI: 1S/C13H13N3OS/c1-16-12(17)11(15-13(16)18)6-8-7-14-10-5-3-2-4-9(8)10/h2-5,7,11,14H,6H2,1H3,(H,15,18)
• Nemzetközi kémiai azonosító kulcs: TXUWMXQFNYDOEZ-UHFFFAOYSA-N

Leírás

Általános leírás

A cell-permeable, potent, and selective blocker of necroptosis (EC₅₀ = 494 nM in FADD-deficient Jurkat cells treated with TNF-α), a nonapoptotic necrotic cell death pathway mediated by death-domain receptors (DRs) that offers neuroprotection in a murine model of ischemic brain injury. Exhibits no effect on DR-induced apoptosis. Also acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect of RIP2 kinase activity. Nec-1 target appears to be a critical common necroptotic step upstream of execution events and downstream of DRs. Inactive control, Nec-1i, is also available (Cat. No. 480066).

A cell-permeable, potent, and selective blocker of necroptosis (EC₅₀ = 494 nM in FADD-deficient Jurkat cells treated with TNF-α), a nonapoptotic necrotic cell death pathway mediated by death-domain receptors (DRs) that offers neuroprotection in a murine model of ischemic brain injury. Exhibits no effect on DR-induced apoptosis. Also acts as a selective and ATP-competitive inhibitor of RIP1 kinase with negligible effect of RIP2 kinase activity. Nec-1 target appears to be a critical common necroptotic step upstream of execution events and downstream of DRs. Inactive control, Nec-1i, is also available (Cat. No. 480066). Also available as a 25 mM solution in DMSO (Cat. No. 505224).

Biokémiai/fiziológiai hatások

Cell permeable: yes

EC50 = 494 nM in blocking necrosis in FADD-deficient Jurkat cells treated with TNF-α

Primary Target
Blocker of necroptosis

Product competes with ATP.

Reversible: no

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Feloldás

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Egyéb megjegyzések

Degterev, A., et al. 2013. Nat. Chem. Biol.9, 192.
Degterev, A., et al. 2012. Cell Death Differ.20, 366.
Christofferson, D.E., et al. 2012. Cell Death Dis.3, e320.
Takahashi, N., et al. 2012. Cell Death Dis.3, e437.
Degterev, A., et al. 2008. Nat. Chem. Biol.4, 313.
Degterev, A., et al. 2005. Nat. Chem. Biol.1, 112.
Muller, A.J., et al. 2005. Nat. Med.11, 312.
Teng, X., et al. 2005. Bioorg. Med. Chem. Lett.15, 5039.

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