Necrostatin-1 - ≥99%, high purity , CAS No.4311-88-0, Inhibitor of indoleamine 2;3-dioxygenase 1;Inhibitor of receptor interacting serine/threonine kinase 1

1 Citations
Item Number
N125522
Grouped product items
SKUSizeAvailabilityPrice Qty
N125522-10mg
10mg
In stock
$58.90
N125522-50mg
50mg
In stock
$177.90
N125522-100mg
100mg
In stock
$224.90
N125522-250mg
250mg
In stock
$506.90
N125522-1g
1g
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,822.90

Potent, specific necroptosis inhibitor

Basic Description

Synonyms5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanyl-3,5-dihydro-4H-imidazol-4-one | 5-(1H-indol-3-ylmethyl)-3-methyl-2-thioxo-4-Imidazolidinone | A826160 | HMS3229H21 | CCG-265032 | HY-15760 | Necrostatin 1 | 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxoimidazolidin-
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsNecrostatin-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
Storage TempStore at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of indoleamine 2;3-dioxygenase 1;Inhibitor of receptor interacting serine/threonine kinase 1
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Necrostatin-1has been used to investigate its effect on the regulation of interleukin (IL)-33 expression during liver injury in mice in vivo and in hepatic stellate cells in vitro.It has also been used as an inhibitor of receptor-interacting protein kinase 1 (RIPK1) in experimental studies.

Associated Targets(Human)

RIPK1 Tchem Receptor-interacting serine/threonine-protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
IDO1 Tchem Indoleamine 2,3-dioxygenase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
THRB Tclin Thyroid hormone receptor beta-1 (7926 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GLA Tclin Alpha-galactosidase A (5444 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK2 Tchem Serine/threonine-protein kinase RIPK2 (1546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TP53 Tchem Cellular tumor antigen p53 (48468 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HL-60 (67320 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HT-29 (80576 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U-937 (7138 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Jurkat (10389 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IDO1 Tchem Indoleamine 2,3-dioxygenase (6650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HSD17B10 Tchem Endoplasmic reticulum-associated amyloid beta-peptide-binding protein (20669 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK1 Tchem Receptor-interacting serine/threonine-protein kinase 1 (1548 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SMN1 Tchem Survival motor neuron protein (34246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RIPK3 Tchem Receptor-interacting serine/threonine-protein kinase 3 (468 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HSP90AA1 Tchem Heat shock protein HSP90 (3606 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
LLC-PK1 (2135 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NIH3T3 (5395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HT-22 (3261 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
L929 (3802 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mapt Microtubule-associated protein tau (6 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name 5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanylideneimidazolidin-4-one
INCHI 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)
InChi Key TXUWMXQFNYDOEZ-UHFFFAOYSA-N
Canonical SMILES CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32
Isomeric SMILES CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32
WGK Germany 3
Alternate CAS 4311-88-0
PubChem CID 2828334
MeSH Entry Terms Nec-1 compound;necrostatin-1
Molecular Weight 259.33

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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8 results found

Lot NumberCertificate TypeDateItem
E2225217Certificate of AnalysisMar 19, 2024 N125522
E2225218Certificate of AnalysisMar 19, 2024 N125522
E2225227Certificate of AnalysisMar 19, 2024 N125522
E2225230Certificate of AnalysisMar 19, 2024 N125522
B2108008Certificate of AnalysisDec 14, 2022 N125522
D2307381Certificate of AnalysisMar 23, 2022 N125522
E2225226Certificate of AnalysisMar 23, 2022 N125522
K2316077Certificate of AnalysisMar 23, 2022 N125522

Chemical and Physical Properties

SolubilitySoluble in DMSO (10-25 mg/ml), 100% ethanol (6 mg/ml), and methanol (5 mg/ml).
SensitivityLight Sensitive;air sensitive;heat sensitive
Melt Point(°C)160.0 - 164.0 °C

Safety and Hazards(GHS)

WGK Germany 3

Related Documents

Citations of This Product

1. Yao Li, Jie Wang, Yaru Li, Jiajia Luo, Fang Liu, Tiantian Chen, Yuting Ji, Hong Yang, Zheng Wang, Yanjun Zhao.  (2023)  Attenuating Uncontrolled Inflammation by Radical Trapping Chiral Polymer Micelles.  ACS Nano,      [PMID:37352508]

References

1. Degterev A, Hitomi J, Germscheid M, Ch'en IL, Korkina O, Teng X, Abbott D, Cuny GD, Yuan C, Wagner G et al..  (2008)  Identification of RIP1 kinase as a specific cellular target of necrostatins..  Nat Chem Biol,  (5): (313-21).  [PMID:18408713]
2. Degterev A, Huang Z, Boyce M, Li Y, Jagtap P, Mizushima N, Cuny GD, Mitchison TJ, Moskowitz MA, Yuan J.  (2005)  Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury..  Nat Chem Biol,  (2): (112-9).  [PMID:16408008]
3. Takahashi N, Duprez L, Grootjans S, Cauwels A, Nerinckx W, DuHadaway JB, Goossens V, Roelandt R, Van Hauwermeiren F, Libert C et al..  (2012)  Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models..  Cell Death Dis,  (3): (e437).  [PMID:23190609]
4. Alegre-Cortés E et al..  (2020)  Toxicity of Necrostatin-1 in Parkinson's Disease Models..  Antioxidants (Basel),  (6):   [PMID:32549347]
5. Li CJ et al..  (2015)  \nSynergistic protection of N-acetylcysteine and ascorbic acid 2-phosphate on human mesenchymal stem cells against mitoptosis, necroptosis and apoptosis.\n.  Sci Rep,  (9819).  [PMID:25909282]
6. Molnár T et al..  (2021)  Caspase-9 acts as a regulator of necroptotic cell death..  FEBS J,  288  (22): (6476-6491).  [PMID:33899329]
7. Tsui KH et al..  (2017)  DHEA protects mitochondria against dual modes of apoptosis and necroptosis in human granulosa HO23 cells..  Reproduction,  154  (2): (101-110).  [PMID:28624766]
8. Lau H et al..  (2020)  Dose-dependent effects of necrostatin-1 supplementation to tissue culture media of young porcine islets..  PLoS One,  15  (12): (e0243506).  [PMID:33284818]
9. Matsuda H et al..  (2017)  HCaRG/COMMD5 inhibits ErbB receptor-driven renal cell carcinoma..  Oncotarget,  (41): (69559-69576).  [PMID:29050225]
10. Bockerstett KA et al..  (2018)  Interleukin-17A Promotes Parietal Cell Atrophy by Inducing Apoptosis..  Cell Mol Gastroenterol Hepatol,  (4): (678-690.e1).  [PMID:29930985]
11. Dallenga T et al..  (2017)  M.\xa0tuberculosis-Induced Necrosis of Infected Neutrophils Promotes Bacterial Growth Following Phagocytosis by Macrophages..  Cell Host Microbe,  22  (4): (519-530.e3).  [PMID:29024644]
12. Yan S et al..  (2021)  Necroptosis pathway blockage attenuates PFKFB3 inhibitor-induced cell viability loss and genome instability in colorectal cancer cells..  Am J Cancer Res,  11  (5): (2062-2080).  [PMID:34094669]
13. Yan B et al..  (2018)  Necrostatin-1 promotes ectopic periodontal tissue like structure regeneration in LPS-treated PDLSCs..  PLoS One,  13  (11): (e0207760).  [PMID:30462730]
14. Lau H et al..  (2019)  Necrostatin-1 supplementation enhances young porcine islet maturation and in vitro function..  Xenotransplantation,    (e12555).  [PMID:31532037]
15. Lau H et al..  (2021)  Necrostatin-1 Supplementation to Islet Tissue Culture Enhances the In-Vitro Development and Graft Function of Young Porcine Islets..  Int J Mol Sci,  22  (16):   [PMID:34445075]
16. Lau H et al..  (2021)  The effects of necrostatin-1 on the in vitro development and function of young porcine islets over 14-day prolonged tissue culture..  Xenotransplantation,  28  (3): (e12667).  [PMID:33438288]
17. Trimova G et al..  (2020)  Tumour necrosis factor alpha promotes secretion of 14-3-3? by inducing necroptosis in macrophages..  Arthritis Res Ther,  22  (24).  [PMID:32051018]
18. Yao Li, Jie Wang, Yaru Li, Jiajia Luo, Fang Liu, Tiantian Chen, Yuting Ji, Hong Yang, Zheng Wang, Yanjun Zhao.  (2023)  Attenuating Uncontrolled Inflammation by Radical Trapping Chiral Polymer Micelles.  ACS Nano,      [PMID:37352508]

Solution Calculators