Necrostatin-1

Modify Date: 2026-07-07 19:04:30

Necrostatin-1 Structure
Necrostatin-1 structure
Common Name Necrostatin-1
CAS Number 4311-88-0 Molecular Weight 259.327
Density 1.4±0.1 g/cm3 Boiling Point 441.9±37.0 °C at 760 mmHg
Molecular Formula C13H13N3OS Melting Point 151ºC
MSDS Chinese USA Flash Point 221.1±26.5 °C

 Use of Necrostatin-1


Necrostatin-1 is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.

 Names

Name 5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanylideneimidazolidin-4-one
Synonym More Synonyms

 Necrostatin-1 Biological Activity

Description Necrostatin-1 is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.
Related Catalog
Target

RIP1 kinase[1]

In Vitro Necrostatin-1 (Nec-1) is a specific and potent small-molecule inhibitor of cell death caused by death-domain receptor (DR) stimulation in the presence of caspase inhibition in multiple cell types. Necrostatin-1 efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors[1]. Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)[2]. The decreased viability of C6 glioma cells caused by 3.0 µM and 6.0 µM shikonin is improved by pretreatment with Necrostatin-1 (Nec-1) to 92.3% and 82.9% at 1.5 h and 84.4% and 78.6% at 3.0 h, respectively. Similarly, the viability of U87 glioma cells is elevated by Necrostatin-1 to 91.6% and 81.5% at 1.5 h, and 81.8% and 71.2% at 3.0 h, respectively[3]. Necrostatin-1 (Nec-1) (30 µM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].
In Vivo Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period[2].
Cell Assay C6 (3×105 cells/well) and U87 (1.5×105 cells/well) glioma cells are seeded onto 96-well microplate and cultured 24 h. PBS is added into the control group and Shikonin is added into experimental group to reach the final concentration. Cellular viability is assessed using an MTT assay after Shikonin treatment at indicated time point. The absorbance value (A) at 570 nm is read using an automatic multi-well spectrophotometer. Two groups of glioma cells from the same cell line are treated with Shikonin at lower or higher concentration, respectively; other two groups of glioma cells are treated 1 h with 100 µM Necrostatin-1 or 40 µM z-VAD-fmk prior to co-incubation with Shikonin at indicated concentration. Additionally, another two groups of glioma cells are treated only with 100 µM Necrostatin-1 or 40 µM Z-VAD-fmk at corresponding time point[3].
Animal Admin Mice[2] 8-10 week old male C57BL/6 mice (average weight approx.23 g) are used. Mice receive intravenous application of 200 μL PBS or radiocontrast media (RCM) via the tail vein. A single dose of Z-VAD-fmk (10 mg/kg body weight) or Necrostatin-1 (1.65 mg/kg body weight) is applied intraperitoneally 15 min. before RCM-injection. Mice are harvested another 24 hours after RCM-application (48 hours after reperfusion). Blood samples are obtained from retroorbital bleeding and serum levels of urea and creatinine are determined.
References

[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.

[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.

[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.

[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.

[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 441.9±37.0 °C at 760 mmHg
Melting Point 151ºC
Molecular Formula C13H13N3OS
Molecular Weight 259.327
Flash Point 221.1±26.5 °C
Exact Mass 259.077942
PSA 80.22000
LogP 1.26
Appearance of Characters solid
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.738
InChIKey TXUWMXQFNYDOEZ-UHFFFAOYSA-N
SMILES CN1C(=O)C(Cc2c[nH]c3ccccc23)NC1=S
Storage condition −20°C
Water Solubility DMSO: >10 mg/mL

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
Risk Phrases 36/37/39
Safety Phrases 36/37/39
RIDADR NONH for all modes of transport
WGK Germany 3
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Necrostatin-1Bioassay

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Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
Name: Tocris HTS for Inhibitors of Aerobactin Synthetase lucA
Source: 23265
External Id: IucA Pilot Assay Tocris Library
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OPM1-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-OC1MY5-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-KMS_34-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_L363-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-keats_OCIMY7-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-MM1R-m4-1
Name: Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
Source: NCGC
Target: N/A
External Id: s-my-mm1s-m4-1
Name: Cell Proliferation Assay Versus the ED40515 IL2 Independent ATL cell lines
Source: NCGC
Target: N/A
External Id: ATLMIPE3-IL2
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 Synonyms

5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-imidazolidinone
Necrostatin-1
5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxoimidazolidin-4-one
Necrostatin 1
MTH-trp
5-indol-3-ylmethyl-3-methyl-2-thioxo-imidazolidin-4-one
Nec-1
Necroptotic Inhibitor,Nec-1
MTH-DL-Tryptophan
methyl-thiohydantoin-tryptophan
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