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Merck
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Documentos clave

480065

Sigma-Aldrich

Necrostatin-1

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

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C13H13N3OS
Número de CAS:
4311-88-0
Peso molecular:
259.33
Número MDL:
MFCD00056916
Código UNSPSC:
12352200
NACRES:
NA.77

Nombre del producto

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).

Nivel de calidad

100

Ensayo

≥95% (HPLC)

Formulario

crystalline solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

yellow

solubilidad

DMSO: 10 mg/mL
methanol: 5 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

cadena SMILES

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)

Clave InChI

TXUWMXQFNYDOEZ-UHFFFAOYSA-N

Descripción general

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).

Acciones bioquímicas o fisiológicas

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

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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.

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Molecules (Basel, Switzerland), 27(13) (2022-07-10)
The use of nanomaterials rationally engineered to treat cancer is a burgeoning field that has reported great medical achievements. Iron-based polymeric nano-formulations with precisely tuned physicochemical properties are an expanding and versatile therapeutic strategy for tumor treatment. Recently, a peculiar
Kana Otsubo et al.
FEBS letters, 594(10), 1586-1595 (2020-01-31)
Autophagy is an intracellular process that regulates the degradation of cytosolic proteins and organelles. Dying cells often accumulate autophagosomes. However, the mechanisms by which necroptotic stimulation induces autophagosomes are not defined. Here, we demonstrate that the activation of necroptosis with
Bolin Hou et al.
Cell death discovery, 8(1), 319-319 (2022-07-14)
The underlying mechanism by which growth factor receptor-bound protein 2 (Grb2) regulates necroptosis remains unexplored. In the present study, we found that rasfonin, a fungal natural product and an activator of necroptosis, enhanced Grb2 binding to receptor-interacting serine/threonine kinase 1
Sasker Grootjans et al.
Nature protocols, 11(8), 1444-1454 (2016-07-16)
Several cell death assays have been developed based on a single biochemical parameter such as caspase activation or plasma membrane permeabilization. Our fluorescent apoptosis/necrosis (FAN) assay directly measures cell death and distinguishes between caspase-dependent apoptosis and caspase-independent necrosis of cells
Peng He et al.
Cell death discovery, 10(1), 255-255 (2024-05-25)
Caspase-8 (Casp8) serves as an initiator of apoptosis or a suppressor of necroptosis in context-dependent manner. Members of the p90 RSK family can phosphorylate caspase-8 at threonine-265 (T265), which can inactivate caspase-8 for bypassing caspase-8-mediated blockade of necroptosis and can
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