Description Features In vitro
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Necrostatin-1

Description Features In vitro
Product Name
Necrostatin-1
CAS No.
4311-88-0
Chemical Name
Necrostatin-1
Synonyms
Nec 1;CS-959;NECROSTATIN-1;MTH-DL-TRYPTOPHAN;IFLAB-BB F0911-6127;Necrostatin-1, >=98%;Necrostatin-1 (Nec-1);Necrostatin-1 USP/EP/BP;Ceftobiprole Impurity 24;NECROSTATIN1; NECROSTATIN 1
CBNumber
CB6776886
Molecular Formula
C13H13N3OS
Formula Weight
259.33
MOL File
4311-88-0.mol
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Necrostatin-1 Property

Melting point:
151℃
Boiling point:
441.9±37.0 °C(Predicted)
Density 
1.40±0.1 g/cm3 (20 ºC 760 Torr)
Flash point:
93.3℃
storage temp. 
-20°C
solubility 
DMSO: >10 mg/mL
form 
solid
pka
9.46±0.40(Predicted)
color 
Pale yellow
Sensitive 
Light Sensitive
Stability:
Stable for 2 years from date of purchase as supplied.? Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
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Safety

Risk Statements 
36/37/39
Safety Statements 
36/37/39
WGK Germany 
3
HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H317May cause an allergic skin reaction

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
N9037
Product name
Necrostatin-1
Purity
≥98% (HPLC)
Packaging
10mg
Price
$196
Updated
2024/03/01
Sigma-Aldrich
Product number
480065
Product name
Necrostatin-1
Packaging
5mg
Price
$144
Updated
2024/03/01
TCI Chemical
Product number
N1174
Product name
Necrostatin-1
Packaging
100MG
Price
$305
Updated
2024/03/01
TCI Chemical
Product number
N1174
Product name
Necrostatin-1
Packaging
25MG
Price
$161
Updated
2021/12/16
Alfa Aesar
Product number
J65341
Product name
Necrostatin-1
Packaging
20mg
Price
$135
Updated
2024/03/01
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Necrostatin-1 Chemical Properties,Usage,Production

Description

Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM in 293T cells.

Features

A powerful tool for characterizing the role of necroptosis with characterized primary target.

In vitro

Necrostatin-1 (1-100 μM) inhibits the autophosphorylation of overexpressed and endogenous RIP1.It is found RIP1 is the primary cellular target responsible for the antinecroptosis activity of Necrostatin-1. Necrostatin-1 efficiently suppresses necroptotic cell death triggered by an array of stimuli in a variety of cell types. Necrostatin-1, previously identified as small-molecule inhibitor of necroptosis, inhibits RIP kinase-induced necroptosis and inhibits TNF-α-induced necroptosis in jurkat cells with EC50 of 490 nM.

Description

Necrostatin-1 (4311-88-0) is an inhibitor of necroptosis (non-apoptotic cell death pathway; EC50 = 494 nM).1 It is an ATP-competitive death domain receptor-associated adaptor kinase (RIP1) inhibitor (EC50 = 182 nM).2 Necrostatin-1 displays a protective effect in a mouse model of ischemic brain injury1, inhibits myocardial cell death and reduces infarct size in various mouse heart models3 and inhibits glutamate-induced oxytosis in HT-22 cells4.

Uses

Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM.

Uses

Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. Necrostatin-1 is an inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells. Necrostatin-1 has been used to investigate the pathological importance of necroptosis in ischemic brain injury and myocardial infarction.

Uses

Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. Necrostatin-1 is an inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells. Necrostatin-1 has been used to investigate the pathological importance of necroptosis in ischemic brain injury and myocardial infarction.

Definition

ChEBI: 5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanylidene-4-imidazolidinone is an organonitrogen compound and an organooxygen compound. It is functionally related to an alpha-amino acid.

Biological Activity

ATP-competitive death domain receptor-associated adaptor kinase (RIP1) allosteric inhibitor (EC 50 = 182 nM). Blocks non-apoptotic cell death via inhibition of a specific cellular pathway, necroptosis, which leads to necrosis (EC 50 = 494 nM). Reduces ischemic brain injury in a mouse model of stroke.

Biochem/physiol Actions

Necrostatin-1(Nec-1) might exhibit therapeutic benefit against patients with traumatic brain injury (TBI). In addition, it might also be used to treat other acute central nervous system (CNS) disorders that feature necroptosis as a mode of cell death. It is extensively used to study the effect of receptor-interacting protein kinase 1 (RIPK1) on cell death and inflammation in experimental disease models. Nec‐1 protects hippocampal (HT‐22) cells from glutamate‐induced oxytosis via increasing cellular glutathione (GSH) levels, decreasing reactive oxygen species production, inhibiting the nuclear translocation of apoptosis‐inducing factor and B-cell lymphoma 2 (Bcl‐2) /adenovirus E1B 19kDa‐interacting protein 3‐related pathways.

in vitro

previous study indicated that necrostatin-1 was a selective allosteric inhibitor of the death domain receptor–associated adaptor kinase rip1 in vitro. in this study, rip1 was found to be the primary cellular target responsible for the antinecroptosis activity of necrostatin-1. in addition, two other necrostatins, necrostatin-3 and necrostatin-5, were also shown to target the rip1 kinase step in the necroptosis pathway, but through different mechanism compared with that of necrostatin-1. the findings established necrostatins as the first-in-class inhibitors of rip1 kinase, the key upstream kinase involved in the activation of necroptosis [2].

in vivo

a previous study was designed to investigate the protective effects and mechanisms of nec-1 in concanavalin a-induced hepatitis in mice. it was found that in nec-1-treated mice the amelioration in liver functions and histopathological changes and the suppression of inflammatory cytokine production were observed. western blotting analyses showed that the expression of tnf-α, ifn-γ, il2, il6, and rip1 was significantly reduced in the nec-1-treated mice, which was further confirmed by immunofluorescence and immunohistochemistry. in addition, autophagosome formation was significantly reduced by nec-1 treatment. these results indicated that nec-1 could prevent concanavalin a -induced liver injury via rip1-related and autophagy-related pathways [3].

IC 50

necrostatin-1 (nec-1), (r)-5-([7-chloro-1h-indol-3-yl]methyl)-3-methylimidazolidine-2,4-dione (nec-1a) (figure 1a) (degterev et al., 2008), exhibited an inhibitory constant (ic50) of 0.32 mm for rip1 [1].

storage

Store at RT

References

1) Degterev, et al. (2005), Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury‘ Nature Chem. Biol., 1 112 2) Degterev et al. (2008) Identification of RIP1 kinase as a specific cellular target of necrostatins; Nature Chem. Biol., 4 313 3) Smith et.al. (2007), Necrostatin: a potentially novel cardioprotective agent?; Cardiovasc. Drugs Ther., 21 227 4) Xu et.al. (2007), Necrostatin-1 protects against glutamate-induced glutathione depletion and caspase-independent cell death in HT-22 cells; J. Neurochem., 103 2004

Necrostatin-1 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Necrostatin-1 manufacturers

Career Henan Chemical Co
Product
Necrostatin-1 4311-88-0
Price
US $5.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
1ton
Release date
2019-09-03

4311-88-0, Necrostatin-1Related Search:


  • Necrostatin-1, >=98%
  • CS-959
  • NECROSTATIN1; NECROSTATIN 1
  • Necrostatin-1 - CAS 4311-88-0 - Calbiochem
  • IFLAB-BB F0911-6127
  • 5-(INDOL-3-YLMETHYL)-3-METHYL-2-THIO-HYDANTOIN
  • NECROSTATIN-1
  • MTH-DL-TRYPTOPHAN
  • MTH-DL-Tryptophan Methylthiohydantoin-DL-tryptophan
  • 5-(1H-INDOL-3-YLMETHYL)-3-METHYL-2-THIOXO-4-IMIDAZOLIDINONE
  • 5-(1H-Indole-3ylmethyl)-3-methyl-2-thioxo-4-imidazolidinone
  • 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-Imidazolidinone, 5-(Indol-3-ylmethyl)-3-methyl-2-thio-hydantoin, MTH-DL-Tryptophan
  • Nec 1
  • Methylthiohydantoin-DL-tryptophan, MTH-DL-tryptophan
  • 4-IMidazolidinone, 5-(1H-indol-3-ylMethyl)-3-Methyl-2-thioxo-
  • 5-((1H-indol-3-yl)Methyl)-3-Methyl-2-thioxoiMidazolidin-4-one
  • 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-imidazolidinone Necrostatin 1
  • Necrostatin 1 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-imidazolidinone
  • Methylthiohydantoin-DL-tryptophan
  • NECROSTATIN1;NECROSTATIN 1;METHYLTHIOHYDANTOIN-DL-TRYPTOPHAN
  • Necrostatin-1 USP/EP/BP
  • Necrostatin-1 (Nec-1)
  • 5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanylideneimidazolidin-4-one
  • Receptor-interacting protein kinases,Inhibitor,RIP kinase,RIPK,Nec 1,Ferroptosis,Necrostatin1,Nec1,Necrostatin-1,inhibit,Autophagy,Indoleamine 2,3-Dioxygenase (IDO)
  • Ceftobiprole Impurity 24
  • 4311-88-0
  • Cell Biology
  • Cell Signaling and Neuroscience
  • Apoptosis and Cell Cycle
  • Apoptosis Inhibitors
  • BioChemical
  • Inhibitors
  • Apoptosis Inhibitors
  • Miscellaneous Signaling
  • Inhibitor