Nec-1s (7-Cl-O-Nec1)

Catalog No.S8641 Synonyms: Necrostatin-1 stable

Nec-1s (7-Cl-O-Nec1) Chemical Structure

Molecular Weight(MW): 277.71

Nec-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.

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Biological Activity

Description Nec-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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MEFs NHq0bnpHfW6ldHnvckBie3OjeR?= NFz4epkzOCEEtV2= NFm1cmIyOCCvaX6= M2\ZS3Rp\SCleXzpcoRzd22jdH;zbZMh[2ynYY\h[4UhcW6mdXPl[EBjgSCWTldOtUBkd3WuZDDi[UBqdmirYnn0[YQh[nliTnXjMVF{Ng>? NUXQR3dYOjh5MEGzO|U>
U118 cells NIPRR|BHfW6ldHnvckBie3OjeR?= MlX3NlAxKM7:TR?= Mn;rUoVkNTG|IILl[JVk\XNiUFmgbY5kd3Kyb4LheIlwdiCrbjDl[IVt\m:|aX7lMZRz\WG2ZXSgWVEyQCClZXzsd{4> NWj0c4JjOjV3OUO5PVQ>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 29527209     


(C)WT and MLKL KO mouse embryonic fibroblasts (MEFs) were treated with necrostatin-1 (Nec-1s), a selective RIPK1 inhibitor, in increasing concentrations, or with DMSO as control, for 1 h followed by incubation with 10% normal human serum (NHS). The lysis percentage was determined by PI inclusion. Results are presented as the mean percentage of lysis ± SD. Statistical analysis showed that MLKL KO MEF is as sensitive to CDC as WT MEF (two-way-ANOVA, P = 0.538). (D) MLKL-silenced K562 cells were treated with Nec-1s at the indicated concentrations and then with antibody diluted 1:18 or 1:15 for scrambled or siRNA-treated cells, respectively, followed by complement (NHS, 50%). CD was measured by PI staining, expressed as a calculated mean percentage ± SD, representing three independent experiments. Statistical analysis showed that CDC of MLKL knocked down cells is as sensitive to Nec-1 as CDC of cells treated with a scrambled siRNA (two-way-ANOVA, P = 0.104).

29527209
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

Animal Research:

[1]

- Collapse
  • Animal Models: TNF-induced SIRS model (Female C57BL/6J WT mice)
  • Formulation: endotoxin-free PBS
  • Dosages: 0.6 mg/kg and 6 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (201.64 mM)
Ethanol 9 mg/mL (32.4 mM)
Water 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.

Chemical Information

Molecular Weight 277.71
Formula

C13H12ClN3O2

CAS No. 852391-15-2
Storage powder
in solvent
Synonyms Necrostatin-1 stable

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID