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MW 259.33 Da, Purity >99%. Potent, specific necroptosis inhibitor (EC50 = 490 nM). Selective allosteric inhibitor of death domain receptor-associated adaptor kinase RIP1 in vitro (EC50 = 182 nM). Caspase independent, programmed necrosis pathway.

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Images

Chemical Structure - Necrostatin-1, necroptosis inhibitor (AB141053), expandable thumbnail
  • Functional Studies - Necrostatin-1, necroptosis inhibitor (AB141053), expandable thumbnail

Publications

Key facts

CAS number

4311-88-0

Purity

> 99%

Form

Solid

Molecular weight

259.33 Da

Molecular formula

C13H13N3OS

PubChem identifier

2828334

Nature

Synthetic

Alternative names

Recommended products

MW 259.33 Da, Purity >99%. Potent, specific necroptosis inhibitor (EC50 = 490 nM). Selective allosteric inhibitor of death domain receptor-associated adaptor kinase RIP1 in vitro (EC50 = 182 nM). Caspase independent, programmed necrosis pathway.

Key facts

Purity

> 99%

PubChem identifier

2828334

Solubility

Soluble in ethanol to 50 mM. Soluble in DMSO to 100 mM.

Biochemical name

5-(1H-indol-3-ylmethyl)-3-methyl-2-thioxo-4-Imidazolidinone

Biological description

Potent, specific necroptosis inhibitor (EC50 = 490 nM). Selective allosteric inhibitor of death domain receptor-associated adaptor kinase RIP1 in vitro (EC50 = 182 nM). Caspase independent, programmed necrosis pathway.

Canonical SMILES

CN1C(=O)C(NC1=S)CC2=CNC3=CC=CC=C32

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)

InChIKey

TXUWMXQFNYDOEZ-UHFFFAOYSA-N

IUPAC name

5-(1H-indol-3-ylmethyl)-3-methyl-2-sulfanylideneimidazolidin-4-one

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

Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

RIP also known as Receptor-Interacting Protein or RIPK1 is a serine/threonine-protein kinase with a mass of approximately 74 kDa. It plays an important role in cell death and survival signaling pathways. RIP is expressed ubiquitously across various tissues indicating its importance in many cellular functions. The protein contains a kinase domain an intermediate domain for protein-protein interactions and a death domain which facilitates its involvement in apoptotic signaling processes.

Biological function summary

Receptor-Interacting Protein Kinase 1 (RIPK1) participates in regulating both necroptosis and apoptosis distinguishing itself as an important mediator in cell death mechanisms. As part of the necrosome complex which includes RIPK3 and MLKL RIPK1 functions in necroptosis—a programmed form of necrosis. This characteristic involvement shows its dual role in maintaining cell fate decisions making it an integral part of immune response and inflammation control.

Pathways

RIPK1 strongly associates with the TNF signaling pathway and NF-kB pathway. Its interaction with TNF receptor 1 (TNFR1) and consequent involvement with TRADD and TRAF2 mediates the signal transduction necessary for the activation of NF-kB leading to transcription of genes involved in survival and inflammation. This connection illustrates its capability to switch between promoting cell survival through NF-kB and facilitating cell death via necroptosis or apoptosis depending on cellular context and cues.

Associated diseases and disorders

RIPK1 plays a significant role in conditions such as inflammatory diseases and neurodegenerative disorders. Its overactivation results in excessive cell death implicated in inflammatory conditions; necrostatin a necroptosis inhibitor targets RIPK1 to potentially mitigate this damage. Furthermore RIPK1's dysregulation links to Alzheimer's disease where it can interact with components like RIPK3 to exacerbate neurodegenerative processes. This relationship underlines the potential of targeting RIPK1 therapeutically to manage inflammation and neurodegeneration.

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2 product images

  • Chemical Structure - Necrostatin-1, necroptosis inhibitor (ab141053), expandable thumbnail

    Chemical Structure - Necrostatin-1, necroptosis inhibitor (ab141053)

    2D chemical structure image of ab141053, Necrostatin-1, necroptosis inhibitor

  • Functional Studies - Necrostatin-1, necroptosis inhibitor (ab141053), expandable thumbnail
    Yan et al PLoS One. 2018 Nov 21;13(11):e0207760. doi: 10.1371/journal.pone.0207760. eCollection 2018. Fig 2. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

    Functional Studies - Necrostatin-1, necroptosis inhibitor (ab141053)

    Necroptosis exists in PDLSCs.

    TEM, a representative normal cell (the cell had a long fusiform, cell membrane structure was complete, the nucleus was round, nucleolus was obvious and center), b representative necroptosis cell (cell membrane ruptured, organelle disappeared, chromatin consolidated and agglutinated, presenting necrotic ultrastructural characteristics), c representative necrosis cell after Nec-1 inhibited (the cell membrane was intact, and the chromatin structure returned to normal).

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