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Necrostatin 2

In vitro necroptosis inhibitor CAS# 852391-19-6

Necrostatin 2

Catalog No. BCC1793----Order now to get a substantial discount!

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Chemical structure

Necrostatin 2

3D structure

Chemical Properties of Necrostatin 2

Cas No. 852391-19-6 SDF Download SDF
PubChem ID 11288934 Appearance Powder
Formula C13H12ClN3O2 M.Wt 277.71
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name (5R)-5-[(7-chloro-1H-indol-3-yl)methyl]-3-methylimidazolidine-2,4-dione
SMILES CN1C(=O)C(NC1=O)CC2=CNC3=C2C=CC=C3Cl
Standard InChIKey WIKGAEMMNQTUGL-SNVBAGLBSA-N
Standard InChI InChI=1S/C13H12ClN3O2/c1-17-12(18)10(16-13(17)19)5-7-6-15-11-8(7)3-2-4-9(11)14/h2-4,6,10,15H,5H2,1H3,(H,16,19)/t10-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Necrostatin 2

DescriptionNecrostatin-2 (Nec-2) is a small molecule inhibitor of  RIPK2 kinase activity
TargetsRIPK2     

Protocol

Kinase Assay [2]
Evaluation of necroptosis inhibitory activity is performed using an FADD-deficient variant of human Jurkat T cells treated for 24 h with TNF-α. Under these conditions the cells underwent necroptosis (the DMSO control had ~40% viability), which is inhibited by Necrostatin 2 (EC50=0.21±0.2 μM) as a positive control. For EC50 value determinations, cells are treated with 10 ng/mL human TNF-α in the presence of increasing concentrations of test compounds (0.029, 0.058, 0.12, 0.23, 0.46, 0.93, 1.9, 3.7, 11.1, 33, and 100 μM) in duplicate for 24 h followed by ATP-based viability assessment. EC50 values±SD are determined from at least two independent experiments[2].

Cell Assay [2]
L929 cells (100000 cells/mL, 100 μL/well in a 96-well plate) are treated with 10 ng/mL human TNF-α or 100 μM zVAD.fmk in the presence of DMSO (control), 30 μM Necrostatin 2, or 8for 24 h at 37°C in a humidified incubator with 5% CO2 followed by ATP-based viability assessment as described in the previous experiment. Stock solutions (30 mM) in DMSO are initially prepared and then diluted with DMSO to give testing solutions. Each sample is done in duplicate. The final DMSO concentration is 0.5%. Cell viability values are adjusted to account for nonspecific toxicity, which in most cases is <10%. The reported cell viability values (%)±SD are determined from two independent experiments[2].

References:
[1]. Teng X, et al. Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40. [2]. Jagtap PG, et al. Structure-activity relationship study of tricyclic necroptosis inhibitors. J Med Chem. 2007 Apr 19;50(8):1886-95. [3]. Teng X, et al. Structure-activity relationship study of novel necroptosis inhibitors. Bioorg Med Chem Lett. 2005 Nov 15;15(22):5039-44.

Necrostatin 2 Dilution Calculator

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Necrostatin 2 Molarity Calculator

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Preparing Stock Solutions of Necrostatin 2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.6009 mL 18.0044 mL 36.0088 mL 72.0176 mL 90.022 mL
5 mM 0.7202 mL 3.6009 mL 7.2018 mL 14.4035 mL 18.0044 mL
10 mM 0.3601 mL 1.8004 mL 3.6009 mL 7.2018 mL 9.0022 mL
50 mM 0.072 mL 0.3601 mL 0.7202 mL 1.4404 mL 1.8004 mL
100 mM 0.036 mL 0.18 mL 0.3601 mL 0.7202 mL 0.9002 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Necrostatin 2

Necrostatin 2 (Nec-2) is a novel and potent necroptosis inhibitor with EC50 of 50 nM. It is an analog of necrostatin 1 (nec-1).

Necroptosis is a mechanism of necrotic cell death induced by apoptotic stimuli in the form of death domain receptor engagement by their respective ligands under conditions where apoptotic execution is prevented. 

Nec-2 is efficacious in an animal model of ischemic stroke. Many Necroptosis inhibitor derivatives are designed for researchers. There is limited record for Nec-2, but some reports are related with other necrostatins. Nec-1, a small-molecule inhibitor of necroptosis, is also a selective allosteric inhibitor of the death domain receptor-associated adaptor kinase RIP1 in vitro.

Reference:
[1].  Teng X, Keys H, Jeevanandam A, Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6836-40.

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Necrostatin 2 is a potent necroptosis inhibitor.

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