Necrostatin 2 racemate (Nec-1s)

Catalog No.S8641 Batch:S864105

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Technical Data

Formula

C13H12ClN3O2
Molecular Weight 277.71 CAS No. 852391-15-2
Solubility (25°C)* In vitro DMSO 55 mg/mL (198.04 mM)
Ethanol 13 mg/mL (46.81 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Necrostatin 2 racemate (Nec-1s, 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S) is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
Targets
RIPK1 [1]
In vitro

Nec-1s is a potent inhibitor of RIPK1 and cellular necroptosis while lacking IDO inhibitory activity[1].
In vivo

Nec-1s is effective in reducing brain injuries. It is a superior inhibitor suitable for use in vivo lacking a paradoxical sensitizing effect in TNF-induced lethality[1].

Nec-1s possesses several advantageous pharmacokinetic and pharmacodynamic characteristics in comparison to Nec-1. Safety profile of Nec-1s is also superior to that of Nec-1 for reduced in vivo and in vitro toxicity[2].

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    BMDMs

  • Concentrations

    50 µM

  • Incubation Time

    6 h

  • Method

    Cells were treated with indicated concentrations of drug.
Animal Study:

[1]
  • Animal Models

    TNF-induced SIRS model (Female C57BL/6J WT mice)

  • Dosages

    0.6 mg/kg and 6 mg/kg

  • Administration

    i.v.

Selleck's Necrostatin 2 racemate (Nec-1s) has been cited by 64 publications

7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] PubMed: 38297130
7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] PubMed: 38297130
The RIPK1 death domain restrains ZBP1- and TRIF-mediated cell death and inflammation [ Immunity, 2024, S1074-7613(24)00221-8] PubMed: 38744293
Inhibition of RIPK1 alleviating vascular smooth muscle cells osteogenic transdifferentiation via Runx2 [ iScience, 2024, 27(2):108766] PubMed: 38318355
Haemolysins are essential to the pathogenicity of deep-sea Vibrio fluvialis [ iScience, 2024, 27(5):109558] PubMed: 38650982
NLRP6 induces RIP1 kinase-dependent necroptosis via TAK1-mediated p38MAPK/MK2 phosphorylation in S. typhimurium infection [ iScience, 2024, 27(4):109339] PubMed: 38500819
Classical apoptotic stimulus, staurosporine, induces lytic inflammatory cell death, PANoptosis [ J Biol Chem, 2024, 300(9):107676] PubMed: 39151726
Slowly progressive cell death induced by GPx4-deficiency occurs via MEK1/ERK2 activation as a downstream signal after iron-independent lipid peroxidation [ J Clin Biochem Nutr, 2024, 74(2):97-107] PubMed: 38510679
NLRP12-PANoptosome activates PANoptosis and pathology in response to heme and PAMPs [ Cell, 2023, 186(13):2783-2801.e20] PubMed: 37267949
NLRP12-PANoptosome activates PANoptosis and pathology in response to heme and PAMPs [ Cell, 2023, 186(13):2783-2801.e20] PubMed: 37267949

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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