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
Molecular Weight: 259.33. Empirical Formula: C13H13N3OS. 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. 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).- UPC:
- 51285903
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5052240001