Nécrostatine-1 (Nec-1) est un inhibiteur puissant de la nécroptose avec un EC50 de 490 nM dans les cellules Jurkat. Nécrostatine-1 inhibe la kinase RIP1 (EC50=182 nM). Nécrostatine-1 est également un IDO inhibiteur.
Necrostatin-1 (Nec-1) ist ein potenter Nekroptose-Inhibitor mit einem EC50 von 490 nM in Jurkat-Zellen. Necrostatin-1 hemmt die RIP1 kinase (EC50=182 nM). Necrostatin-1 ist auch ein IDO-Hemmer.
Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor.
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Necrostatin-1 Chemical Structure
CAS No. : 4311-88-0
This product is a controlled substance and not for sale in your territory.
Based on 293 publication(s) in Google Scholar
Other Forms of Necrostatin-1:
Necrostatin-1 (inactive control)
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Necrostatin-1 purchased from MedChemExpress. Usage Cited in:
Braz J Med Biol Res. 2018 Nov 23;52(1):e7844.
[Abstract]
Representative western blot graphs showing the effects of tumor necrosis factor-α (TNF-α) on the protein expression levels of specific marker proteins receptor interacting protein kinase (RIPK3), mixed lineage kinase domain-like protein (MLKL) and p-MLKL, caspase 3 and cleaved caspase 3, and b-actin in MC3T3-E1 cells with TNF-α, Nec-1 or Z-IETD-FMK treatment.
Nec-1 treatment inhibits RIP1-RIP3, p-DRP1 activation and reduces the expression of NLRP3 and cleaved caspase-1 at 24 h after SAH. Representative Western blots showing levels of RIP1, RIP3, p-DRP1, DRP1, NLRP3 and cleaved caspase-1.
Necrostatin-1 purchased from MedChemExpress. Usage Cited in:
Sci Rep. 2017 Nov 23;7(1):16111.
[Abstract]
RIP1 does not mediate TNFα-induced apoptosis in RIP3 knockdown L929 cells. Nec-1 does not block the TNFα-induced death of RIP3 knockdown L929 cells. The cells are infected with the RIP3 shRNA or the negative control shRNA lentivirus, and western blotting is performed to determine RIP3 knockdown efficiency.
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Voir tous les produits spécifiques à Isoform RIP kinase:
Voir toutes les isoformes
RIPK1 RIPK2 RIPK3
Voir tous les produits spécifiques à Isoform Indoleamine 2,3-Dioxygenase (IDO):
Voir toutes les isoformes
IDO1 IDO2 IDO
Description
Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor[1].
IC50 & Target
EC50: 182 nM (RIP1 kinase)[1]
Cellular Effect
Cell Line
Type
Value
Description
References
Jurkat
IC50
494 nM
Compound: 1, Nec-1
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
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
[PMID: 16408008]
Sf9
IC50
182 nM
Compound: Necrostatin-1
Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method
Inhibition of recombinant human GST-fused RIPK1 (1 to 497 residues) expressed in baculovirus infected insect Sf9 cells in presence of 32P-gamma-ATP after 30 mins by autoradiogram-based Western blot method
[PMID: 28280261]
In Vitro
Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors[1].
Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)[2].
Necrostatin-1 (Nec-1) (30 μM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Necrostatin-1 Related Antibodies
In Vivo
Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Masse moléculaire
259.33
Formule
C13H13N3OS
CAS No.
4311-88-0
Appearance
Solid
Color
Light yellow to yellow
SMILES
O=C(C(CC1=CNC2=C1C=CC=C2)N3)N(C)C3=S
Livraison
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (482.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
3.8561 mL
19.2805 mL
38.5609 mL
5 mM
0.7712 mL
3.8561 mL
7.7122 mL
10 mM
0.3856 mL
1.9280 mL
3.8561 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% (50% EtOH 50% Cremophor EL) 90% Saline
Solubility: 1.67 mg/mL (6.44 mM); Suspended solution; Need ultrasonic
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 12.5 mg/mL (48.20 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.
[Content Brief]
[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.
[Content Brief]
[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.
[Content Brief]
[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.
[Content Brief]
[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.
[Content Brief]
Test cellulaire
[3]
C6 (3×105 cells/well) and U87 (1.5×105 cells/well) glioma cells are seeded onto 96-well microplate and cultured 24 h. PBS is added into the control group and Shikonin is added into experimental group to reach the final concentration. Cellular viability is assessed using an MTT assay after Shikonin treatment at indicated time point. The absorbance value (A) at 570 nm is read using an automatic multi-well spectrophotometer. Two groups of glioma cells from the same cell line are treated with Shikonin at lower or higher concentration, respectively; other two groups of glioma cells are treated 1 h with 100 µM Necrostatin-1 or 40 µM z-VAD-fmk prior to co-incubation with Shikonin at indicated concentration. Additionally, another two groups of glioma cells are treated only with 100 µM Necrostatin-1 or 40 µM Z-VAD-fmk at corresponding time point[3].
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale
Mice[2]
8-10 week old male C57BL/6 mice (average weight approx.23 g) are used. Mice receive intravenous application of 200 μL PBS or radiocontrast media (RCM) via the tail vein. A single dose of Z-VAD-fmk (10 mg/kg body weight) or Necrostatin-1 (1.65 mg/kg body weight) is applied intraperitoneally 15 min. before RCM-injection. Mice are harvested another 24 hours after RCM-application (48 hours after reperfusion). Blood samples are obtained from retroorbital bleeding and serum levels of urea and creatinine are determined.
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références
[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.
[Content Brief]
[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.
[Content Brief]
[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.
[Content Brief]
[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.
[Content Brief]
[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.
[Content Brief]
[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.
[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.
[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.
[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.
[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
Necrostatin-14311-88-0Nec-1Necrostatin1Necrostatin 1Nec1Nec 1RIP kinaseAutophagyIndoleamine 2,3-Dioxygenase (IDO)FerroptosisReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit
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