5.05224

Necrostatin-1

InSolution, ≥95%, 25 mM in DMSO, required for the biosynthesis of sialic acid-containing complex carbohydrates

• Synonym(s): InSolution Necrostatin-1, 5-((1H-Indol-3-yl)methyl)-3-methyl-2-thioxoimidazolidin-4-one; 5-(Indol-3-ylmethyl)-(2-thio-3-methyl)hydantoin, MTH-Trp, Methyl-thiohydantoin-tryptophan, Nec-1, Nec1, Necrosome Inhibitor I, RIP1 Inhibitor I, RIPK 1 Inhibitor I, Receptor-Interacting Protei, Necrosis Inhibitor II, 5-((1H-Indol-3-yl)methyl)-3-methyl-2-thioxoimidazolidin-4-one; 5-(Indol-3-ylmethyl)-(2-thio-3-methyl)hydantoin, MTH-Trp, Methyl-thiohydantoin-tryptophan, Nec-1, Nec1, Necrosome Inhibitor I, RIP1 Inhibitor I, RIPK 1 Inhibitor I, Receptor-Interacting Protein 1 Inhibitor I
• Empirical Formula (Hill Notation): C₁₃H₁₃N₃OS
• Molecular Weight: 259.33
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• storage temp.: −70°C

Description

General description

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 on 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).

Biochem/physiol Actions

Cell permeable: yes

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

A 25 mM (10 mg/1.54 ml) sterile-filtered solution of Necrostatin-1 (Cat. No. 480065) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 2
• Flash Point(F): 188.6 °F - (refers to pure substance)
• Flash Point(C): 87 °C - (refers to pure substance)