Necrostatin 2 racemate (Nec-1s)

Synonyms: 7-Cl-O-Nec1, Necrostatin-1 stable, Necrostatin 1S

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.

Necrostatin 2 racemate (Nec-1s) Chemical Structure

Necrostatin 2 racemate (Nec-1s) Chemical Structure

CAS No. 852391-15-2

Purity & Quality Control

Products often used together with Necrostatin 2 racemate (Nec-1s)

Fer-1 (Ferrostatin-1)


Necrostatin 2 and Ferrostatin-1 inhibit the BAY-induced reduction in cell viability to a similar extent in melanoma cells.

Basit F, et al. Cell Death Dis. 2017 Mar 30;8(3):e2716.

Z-VAD-FMK


Necrostatin 2 racemate and Z-VAD-FMK partially reduce cell death in response to heme plus Pam3 in WT bone marrow-derived macrophages.

Sundaram B, et al. Cell. 2023 Jun 22;186(13):2783-2801.e20.

GSK'872


Necrostatin 2 racemate and GSK'872 as inhibitors of apoptosis do not induce cell death in trans-differentiated 3T3-L1 cells.

Gautheron J, et al. Nat Commun. 2016 Jun 21;7:11869.

Lipopolysaccharides


Necrostatin 2 racemate abolishes the increase in TNFalpha synthesis by LPS with zVAD in RIPK1 D138N cells.

Najjar M, et al. Immunity. 2016 Jul 19;45(1):46-59.

Necrostatin-1


Necrostatin 2 racemate and Necrostatin-1 exert neuroprotective and anti-inflammatory effects in MPTP-induced PD mice.

Kim DY, et al. Cells. 2023 Jan 26;12(3):417.

Necrostatin 2 racemate (Nec-1s) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U118 cells Function assay 200 μM Nec-1s reduces PI incorporation in edelfosine-treated U118 cells. 25593994
MEFs Function assay 20 µM 10 min The cylindromatosis cleavage induced by TNFα could be inhibited by Nec-1s. 28701375
Jurkat Function assay 30 hrs Inhibition of death receptor signaling mediated necroptotic cell death in human Jurkat cell deficient in FADD assessed as cell viability after 30 hrs by ATP based viability assay in presence of TNFalpha, IC50 = 0.206 μM. 16408008
Jurkat Function assay Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha, EC50 = 0.21 μM. 16153840
Click to View More Cell Line Experimental Data

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
In vitro

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

Cell Research Cell lines BMDMs
Concentrations 50 µM
Incubation Time 6 h
Method

Cells were treated with indicated concentrations of drug.

Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 29527209
In Vivo
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].

Animal Research Animal Models TNF-induced SIRS model (Female C57BL/6J WT mice)
Dosages 0.6 mg/kg and 6 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 277.71 Formula

C13H12ClN3O2

CAS No. 852391-15-2 SDF --
Smiles CN1C(=O)C(NC1=O)CC2=CNC3=C2C=CC=C3Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 56 mg/mL ( (201.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 56 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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