2. Apoptosis Autophagy Metabolic Enzyme/Protease
  3. RIP kinase Autophagy Indoleamine 2,3-Dioxygenase (IDO) Ferroptosis
  4. Necrostatin-1

Necrostatin-1  (Synonyms: Nec-1)

Cat. No.: HY-15760 Purity: 99.89%
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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.

For research use only. We do not sell to patients.

Necrostatin-1 Chemical Structure

Necrostatin-1 Chemical Structure

CAS No. : 4311-88-0

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10 mM * 1 mL in DMSO
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Based on 281 publication(s) in Google Scholar

Other Forms of Necrostatin-1:

Necrostatin-1 Related Antibodies

Top Publications Citing Use of Products

278 Publications Citing Use of MCE Necrostatin-1

WB

    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.

    Necrostatin-1 purchased from MedChemExpress. Usage Cited in: Exp Neurol. 2017 Sep;295:116-124.  [Abstract]

    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.

    View All RIP kinase Isoform Specific Products:

    View All Isoforms
    RIPK1 RIPK2 RIPK3

    View All Indoleamine 2,3-Dioxygenase (IDO) Isoform Specific Products:

    View All Isoforms
    IDO1 IDO2 IDO

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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]
    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.
    Molecular Weight

    259.33

    Formula

    C13H13N3OS
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C(CC1=CNC2=C1C=CC=C2)N3)N(C)C3=S
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    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
    Concentration Solvent Mass 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
    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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (8.02 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO 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)

      Solubility: ≥ 2.08 mg/mL (8.02 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO 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.

    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.
     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.
    Purity & Documentation

    Purity: 99.89%

    COA (254 KB) RP-HPLC (242 KB) Elemental Analysis Report (112 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration

    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 has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.8561 mL 19.2805 mL 38.5609 mL 96.4023 mL
    5 mM 0.7712 mL 3.8561 mL 7.7122 mL 19.2805 mL
    10 mM 0.3856 mL 1.9280 mL 3.8561 mL 9.6402 mL
    15 mM 0.2571 mL 1.2854 mL 2.5707 mL 6.4268 mL
    20 mM 0.1928 mL 0.9640 mL 1.9280 mL 4.8201 mL
    25 mM 0.1542 mL 0.7712 mL 1.5424 mL 3.8561 mL
    30 mM 0.1285 mL 0.6427 mL 1.2854 mL 3.2134 mL
    40 mM 0.0964 mL 0.4820 mL 0.9640 mL 2.4101 mL
    50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9280 mL
    60 mM 0.0643 mL 0.3213 mL 0.6427 mL 1.6067 mL
    80 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2050 mL
    100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9640 mL
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    Necrostatin-1 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      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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