MW 461.5 Da, Purity >98%. Potent, selective necroptosis inhibitor (IC50 = 0.2 μM). MLKL blocker. Selectively blocks necrosis downstream of RIP3 activation. Shows selective antinecrotic effects.
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- Oncology reports 50:2023Circular RNA circBLNK promotes osteosarcoma progression and inhibits ferroptosis in osteosarcoma cells by sponging miR‑188‑3p and regulating GPX4 expression.Applications:Unspecified applicationReactive species:Unspecified reactive speciesZhongjun Li,Yi Luo,Chunbo Wang,Dunxin Han,Weiping SunPubMed 37711054
- iScience 26:1065232023Progesterone prevents HGSOC by promoting precancerous cell pyroptosis via inducing fibroblast paracrine.Applications:Unspecified applicationReactive species:Unspecified reactive speciesNayiyuan Wu,Xiaoye Zhang,Zhibin Wang,Xiu Zhang,Chao Fang,He Li,Miaochen Zhu,Ying Wang,Qianjin Liao,Tang-Yuan Chu,Jing WangPubMed 37123232
- iScience 25:1051182022Inhibition of the pseudokinase MLKL alters extracellular vesicle release and reduces tumor growth in glioblastoma.Applications:Unspecified applicationReactive species:Unspecified reactive speciesGwennan André-Grégoire,Clément Maghe,Tiphaine Douanne,Sara Rosińska,Fiorella Spinelli,An Thys,Kilian Trillet,Kathryn A Jacobs,Cyndie Ballu,Aurélien Dupont,Anne-Marie Lyne,Florence M G Cavalli,Ignacio Busnelli,Vincent Hyenne,Jacky G Goetz,Nicolas Bidère,Julie GavardPubMed 36185361
- Translational oncology 13:372-3822019Epigenetic Regulation of RIP3 Suppresses Necroptosis and Increases Resistance to Chemotherapy in NonSmall Cell Lung Cancer.Applications:Unspecified applicationReactive species:Unspecified reactive speciesQiong Wang,Peipei Wang,Li Zhang,Mathewos Tessema,Lang Bai,Xiuling Xu,Qin Li,Xuelian Zheng,Bryanna Saxton,Wenshu Chen,Randy Willink,Zhiping Li,Lin Zhang,Steven A Belinsky,Xia Wang,Bin Zhou,Yong LinPubMed 31887632
- Molecular brain 12:782019miR-212-5p attenuates ferroptotic neuronal death after traumatic brain injury by targeting Ptgs2.Applications:Unspecified applicationReactive species:Unspecified reactive speciesXiao Xiao et. al.PubMed 31533781
- Journal of cellular and molecular medicine 23:7349-73592019Sigma-1 receptor protects against ferroptosis in hepatocellular carcinoma cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTao Bai et. al.PubMed 31507082
- Journal of immunology (Baltimore, Md. : 1950) 203:736-7482019The Pyroptotic Cell Death Effector Gasdermin D Is Activated by Gout-Associated Uric Acid Crystals but Is Dispensable for Cell Death and IL-1β Release.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMaryam Rashidi et. al.PubMed 31209100
- Nature communications 9:44572018A FRET biosensor for necroptosis uncovers two different modes of the release of DAMPs.Applications:Unspecified applicationReactive species:Unspecified reactive speciesShin Murai et. al.PubMed 30367066
- Frontiers in immunology 9:3062018Receptor-Interacting Protein Kinases 1 and 3, and Mixed Lineage Kinase Domain-Like Protein Are Activated by Sublytic Complement and Participate in Complement-Dependent Cytotoxicity.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMichal Lusthaus et. al.PubMed 29527209
- Cell death and differentiation 25:1457-14722018miR-137 regulates ferroptosis by targeting glutamine transporter SLC1A5 in melanoma.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMeiying Luo et. al.PubMed 29348676
Key facts
- CAS number
- 432531-71-0
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 461.5 Da
- Molecular formula
- C18H15N5O6S2
- PubChem identifier
- 1566236
- Nature
- Synthetic
Target data
Alternative names
9130019I15Rik, FLJ34389, MLKL_HUMAN, Mixed lineage kinase domain like, Mixed lineage kinase domain like pseudokinase, Mixed lineage kinase domain-like protein, hMLKL
Recommended products
MW 461.5 Da, Purity >98%. Potent, selective necroptosis inhibitor (IC50 = 0.2 μM). MLKL blocker. Selectively blocks necrosis downstream of RIP3 activation. Shows selective antinecrotic effects.
Key facts
- CAS number
- 432531-71-0
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 461.5 Da
- Molecular formula
- C18H15N5O6S2
- PubChem identifier
- 1566236
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 25 mM.
- Biochemical name
- Necrosulfonamide
- Biological description
Potent, selective necroptosis inhibitor (IC50 = 0.2 μM). MLKL blocker. Selectively blocks necrosis downstream of RIP3 activation. Shows selective antinecrotic effects.
- Canonical SMILES
- COC1=NC=CN=C1NS(=O)(=O)C2=CC=C(C=C2)NC(=O)C=CC3=CC=C(S3)[N+](=O)[O-]
- Isomeric SMILES
- COC1=NC=CN=C1NS(=O)(=O)C2=CC=C(C=C2)NC(=O)/C=C/C3=CC=C(S3)[N+](=O)[O-]
- InChI
- InChI=1S/C18H15N5O6S2/c1-29-18-17(19-10-11-20-18)22-31(27,28)14-6-2-12(3-7-14)21-15(24)8-4-13-5-9-16(30-13)23(25)26/h2-11H,1H3,(H,19,22)(H,21,24)/b8-4+
- InChIKey
- FNPPHVLYVGMZMZ-XBXARRHUSA-N
- IUPAC name
- (E)-N-[4-[(3-methoxypyrazin-2-yl)sulfamoyl]phenyl]-3-(5-nitrothiophen-2-yl)prop-2-enamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°C
- Storage information
- It is important to note that this product is reported to be light sensitive, Store in the dark, Store under desiccating conditions
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
MLKL also known as mixed lineage kinase domain-like protein plays a critical role in the process of necroptosis a form of programmed cell death. The MLKL protein has a molecular weight of approximately 54 kDa. The protein exists mainly within the cytoplasm but translocates to the plasma membrane during cell death execution. Expression of MLKL happens in various tissues indicating its wide biological importance. Phosphorylation of MLKL often referred to as p-MLKL is key to triggering its activity marking the transition from an inactive to an active state during necroptosis.
- Biological function summary
The MLKL protein acts as an executioner of cell death by forming a complex that disrupts the plasma membrane integrity. This process is downstream of receptor-interacting serine/threonine-protein kinase 3 (RIPK3) which phosphorylates MLKL to form the active necrosome complex. Active MLKL oligomerizes and migrates towards the inner leaflet of the plasma membrane binding to phosphatidylinositol phosphates which assists in pore formation and cellular rupture. The ability to measure MLKL activity levels such as via MLKL ELISA kits is important for understanding necrotic processes in detailed studies.
- Pathways
MLKL is integrally involved in the necroptotic pathway alongside RIPK1 and RIPK3 which are key initiators of necroptosis. Phosphorylated MLKL acts downstream of RIPK3 resulting in cell death without caspase activation distinguishing necroptosis from apoptosis. MLKL and RIPK3 are tightly linked within this pathway with MLKL phosphorylation serving as a vital event for the execution phase. The necroptosis pathway is part of larger networks including inflammatory response pathways highlighting the importance of MLKL's role beyond sheer cell death.
- Associated diseases and disorders
MLKL has been implicated in various inflammatory conditions and neurodegenerative diseases. The dysregulation of necroptosis can contribute to disorders such as inflammatory bowel disease and amyotrophic lateral sclerosis. In inflammatory bowel disease increased levels of p-MLKL might lead to excessive cell death exacerbating inflammation. Similarly in neurodegenerative disorders the harmful activation of MLKL may accelerate neuronal cell death. Key interactions with proteins like RIPK3 and RIPK1 highlight MLKL's involvement in these pathological processes making it a potential target for therapeutic intervention.
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Chemical Structure - Necrosulfonamide, necroptosis inhibitor (ab143839)
2D chemical structure image of ab143839, Necrosulfonamide, necroptosis inhibitor
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