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Inhibits necroptosis
BML-AP309-0020 20 mg 139.00 USD
BML-AP309-0100 100 mg 443.00 USD
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Replaces Prod. #: ALX-430-136

Necrostatin-1 inhibits necroptosis, a non-apoptotic cell death pathway. Inhibits the loss of mitochondrial membrane potential in TNFα-treated Jurkat cells (EC50=490 nM). Does not inhibit FAS-induced apoptosis and has no effect on apoptotic morphology. It displays a pronounced protective effect in a mouse model of ischemic brain injury and inhibits myocardial cell death. Inhibits RIP1 kinase the key upstream kinase involved in the activation of necroptosis (EC50=180nM).

Product Details

Alternative Name:Methylthiohydantoin-DL-tryptophan
Purity:≥98% (TLC)
Appearance:Yellow solid.
Solubility:Soluble in DMSO (20mg/ml) or 100% ethanol (5mg/ml).
Shipping:Ambient Temperature
Long Term Storage:Ambient
Use/Stability:Stock solutions are stable for up to 3 months when stored at -20°C.
Handling:Protect from light.
Regulatory Status:RUO - Research Use Only
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Product Literature References

Lysosome‑targeted drug combination induces multiple organelle dysfunctions and non‑canonical death in pancreatic cancer cells: S. Suzuki, et al.; Oncol. Rep. 47, 40 (2022), Abstract;
ROS-mediated activation of p38 protects hepatocellular carcinoma cells from caspase-independent death elicited by lysosomal damage: S. Castelli, et al.; Biochem. Pharmacol. 198, 114983 (2022), Abstract;
TRAIL receptors promote constitutive and inducible IL-8 secretion in non-small cell lung carcinoma: F. Favaro, et al.; Cell Death Dis. 13, 1046 (2022), Abstract;
Elesclomol-induced increase of mitochondrial reactive oxygen species impairs glioblastoma stem-like cell survival and tumor growth: M. Buccarelli, et al.; J. Exp. Clin. Cancer Res. 40, 228 (2021), Abstract;
Induction of synergistic non‑apoptotic cell death by simultaneously targeting proteasomes with bortezomib and histone deacetylase 6 with ricolinostat in head and neck tumor cells: K. Hattori, et al.; Oncol. Lett. 22, 680 (2021), Abstract;
RIP1 kinase inactivation protects against acetaminophen-induced acute liver injury in mice: Y. Yi, et al.; Free Radic. Biol. Med. 174, 57 (2021), Abstract;
TNF-induced necroptosis initiates early autophagy events via RIPK3-dependent AMPK activation, but inhibits late autophagy: W. Wu, et al.; Autophagy 17, 3992 (2021), Abstract;
Beclin 1 Functions as a Negative Modulator of MLKL Oligomerisation by Integrating Into the Necrosome Complex: J. Seo, et al.; Cell Death Differ. 27, 3065 (2020), Abstract; Full Text
Caspase-8, receptor-interacting protein kinase 1 (RIPK1), and RIPK3 regulate retinoic acid-induced cell differentiation and necroptosis: M. Someda, et al.; Cell Death Differ. 27, 1539 (2020), Abstract; Full Text
Docosahexaenoic Acid Protection Against Palmitic Acid-Induced Lipotoxicity in NGF Differentiated PC12 Cells Involves Enhancement of Autophagy and Inhibition of Apoptosis and Necroptosis: M.L. Montero, et al.; J. Neurochem. 155, 559 (2020), Abstract; Full Text
Molecular bases for HOIPINs-mediated inhibition of LUBAC and innate immune responses: D. Oikawa, et al.; Commun. Biol. 3, 163 (2020), Abstract; Full Text
Cathepsin G inhibition by serpinb1 and serpinb6 prevents programmed necrosis in neutrophils and monocytes and reduces GSDMD-driven inflammation: S.S. Burgener, et al.; Cell Rep. 27, 3646 (2019), Abstract;
Ferroptosis in Neurons and Cancer Cells Is Similar But Differentially Regulated by Histone Deacetylase Inhibitors: M. Zille, et al.; eNeuro 6, ENEURO.0263-18.2019 (2019), Abstract; Full Text
Kinase-Based Screening of Marine Natural Extracts Leads to the Identification of a Cytotoxic High Molecular Weight Metabolite from the Mediterranean Sponge Crambe tailliezi: T.N. Nguyen, et al.; Mar. Drugs 17, 569 (2019), Abstract; Full Text
Ubiquitination of RIPK1 suppresses programmed cell death by regulating RIPK1 kinase activation during embryogenesis: X. Zhang, et al.; Nat. Commun. 10, 4158 (2019), Abstract; Full Text
Cylindromatosis mediates neuronal cell death in vitro and in vivo: G.K. Ganjam, et al.; Cell Death Differ. 25, 1394 (2018), Abstract; Full Text
Cold-inducible RNA-binding protein through TLR4 signaling induces mitochondrial DNA fragmentation and regulates macrophage cell death after trauma: Z. Li, et al.; Cell Death Dis. 8, e2775 (2017), Abstract; Full Text
Glucose Deprivation Induces ATF4-Mediated Apoptosis through TRAIL Death Receptors: R. Iurlaro, et al.; Mol. Cell. Biol. 37, e00479-16 (2017), Abstract; Full Text
The anti-myeloma activity of bone morphogenetic protein 2 predominantly relies on the induction of growth arrest and is apoptosis-independent: C. Lagler, et al.; PLoS One 12, e0185720 (2017), Application(s): Jurkat A3 cells, Abstract; Full Text
Caspase-3 Deletion Promotes Necrosis in Atherosclerotic Plaques of ApoE Knockout Mice: M.O. Grootaert, et al.; Oxid. Med. Cell Longev. 2016, 3087 (2016), Application(s): PI labeling experiements, Abstract; Full Text
Inhibition of caspases primes colon cancer cells for 5-fluorouracil-induced TNF-α-dependent necroptosis driven by RIP1 kinase and NF-κB: M. Oliver Metzig, et al.; Oncogene 35, 3399 (2016), Application(s): Cell culture , Abstract;
Macrolide Antibiotics Exhibit Cytotoxic Effect under Amino Acid-Depleted Culture Condition by Blocking Autophagy Flux in Head and Neck Squamous Cell Carcinoma Cell Lines: K. Hirasawa, et al.; PLoS One 11, e0164529 (2016), Abstract; Full Text
MLKL and FADD Are Critical for Suppressing Progressive Lymphoproliferative Disease and Activating the NLRP3 Inflammasome: X. Zhang, et al.; Cell Rep. 16, 3247 (2016), Application(s): Necroptosis inhibition in WT mouse dermal fibroblasts, Abstract;
Molecular features of the cytotoxicity of an NHE inhibitor: Evidence of mitochondrial alterations, ROS overproduction and DNA damage: F. Aredia, et al.; BMC Cancer 16, 851 (2016), Application(s): Colon carcinoma HCT-116 cells , Abstract; Full Text
Retinal pigment epithelial cell necroptosis in response to sodium iodate: J. Hanus, et al.; Cell Death Discov. 2, 16054 (2016), Application(s): Cell culture, transfection, treatments, and MTT assay (human cells), Abstract; Full Text
Simultaneous induction of apoptosis and necroptosis by Tanshinone IIA in human hepatocellular carcinoma HepG2 cells: C.Y. Lin, et al.; Cell Death Discov. 2, 16065 (2016), Application(s): Cell viability assay, flow cytometry, cytotoxicity assay, immunoprecipitation and western blot; with human hepatoma cell line HepG2, Abstract; Full Text
The Autophagy Machinery Controls Cell Death Switching between Apoptosis and Necroptosis: M.L. Goodall, et al.; Dev. Cell 37, 337 (2016), Abstract; Full Text
The Different Effects of Atorvastatin and Pravastatin on Cell Death and PARP Activity in Pancreatic NIT-1 Cells: Y.H. Chen, et al.; J. Diabetes Res. 2016, 1828071 (2016), Abstract;
Differential roles of RIPK1 and RIPK3 in TNF-induced necroptosis and chemotherapeutic agent-induced cell death: K. Moriwaki, et al.; Cell Death Dis. 6, e1636 (2015), Application(s): Cell Culture, Abstract; Full Text
Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via Ivermectin induces a non-apoptotic and inflammatory form of cancer cell death: D. Draganov, et al.; Sci. Rep. 5, 16222 (2015), Abstract; Full Text
Oxaliplatin triggers necrosis as well as apoptosis in gastric cancer SGC-7901 cells: P. Wu, et al.; Biochem. Biophys. Res. Commun. 460, 183 (2015), Application(s): Cell Culture, Abstract;
Toxin-Induced Necroptosis Is a Major Mechanism of Staphylococcus aureus Lung Damage: K. Kitur, et al.; PLoS Pathog. 11, e1004820 (2015), Application(s): Cell Culture, Abstract; Full Text
ZFP36 stabilizes RIP1 via degradation of XIAP and cIAP2 thereby promoting ripoptosome assembly: T. Selmi, et al.; BMC Cancer 15, 357 (2015), Application(s): Cell Culture, Abstract; Full Text
A novel role for the apoptosis inhibitor ARC in suppressing TNFα-induced regulated necrosis: G. Kung, et al.; Cell Death Differ. 21, 634 (2014), Abstract;
Betulinic acid-induced mitochrondria-dependent cell death is counter balanced by an autophagic salvage: L. Potze, et al.; Cell Death Dis. 5, e1169 (2014), Abstract; Full Text
TRAF2 inhibits TRAIL- and CD95L-induced apoptosis and necroptosis: I. Karl, et al.; Cell Death Dis. 5, e1444 (2014), Abstract; Full Text
The Isopeptidase Inhibitor G5 Triggers a Caspase-independent Necrotic Death in Cells Resistant to Apoptosis: A COMPARATIVE STUDY WITH THE PROTEASOME INHIBITOR BORTEZOMIB: A. Fontanini et al.; J. Biol. Chem. 284, 8369 (2009), Abstract;
Identification of RIP1 kinase as a specific cellular target of necrostatins: A. Degterev, et al.; Nat. Chem. Biol. 4, 313 (2008), Abstract;
Chemical genetic approaches to probing cell death: B.R. Stockwell & N.M. Gangadhar; Curr. Opin. Chem. Biol. 11, 83 (2007), Abstract;
Clinical aspects of indoleamine 2,3-dioxygenase (IDO)-initiated tryptophan metabolism: IDO is a target of drug discovery for various diseasea: O. Takikawa; Int. Congr. Ser. 1304, 290 (2007),
Necrostatin-1 protects against glutamate-induced glutathione depletion and caspase-independent cell death in HT-22 cells: X. Xu et al.; J. Neurochem. 103, 2004 (2007), Abstract;
Necrostatin: a potentially novel cardioprotective agent?: C.C. Smith et al.; Cardiovasc. Drugs Ther. 21, 227 (2007), Abstract;
Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury: A. Degterev, et al.; Nat. Chem. Biol. 1, 112 (2005), Abstract;
Inhibition of indoleamine 2,3-dioxygenase, an immunoregulatory target of the cancer suppression gene Bin1, potentiates cancer chemotherapy: A.J. Muller et al.; Nat. Med. 11, 312 (2005), Abstract;

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