1. Apoptosis
    Autophagy
  2. RIP kinase
    Autophagy

Necrostatin-1 (Synonyms: Nec-1)

Cat. No.: HY-15760 Purity: 99.20%
Handling Instructions

Necrostatin-1 (Nec-1) is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.

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

Necrostatin-1 Chemical Structure

Necrostatin-1 Chemical Structure

CAS No. : 4311-88-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

    Necrostatin-1 purchased from MCE. Usage Cited in: Exp Neurol. 2017 Sep;295:116-124.

    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 MCE. Usage Cited in: Sci Rep. 2017 Nov 23;7(1):16111.

    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.

    Necrostatin-1 purchased from MCE. Usage Cited in: Braz J Med Biol Res. 2018 Nov 23;52(1):e7844.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Necrostatin-1 (Nec-1) is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.

    IC50 & Target

    RIP1 kinase[1]

    In Vitro

    Necrostatin-1 (Nec-1) is a specific and potent small-molecule inhibitor of cell death caused by death-domain receptor (DR) stimulation in the presence of caspase inhibition in multiple cell types. Necrostatin-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]. The decreased viability of C6 glioma cells caused by 3.0 µM and 6.0 µM shikonin is improved by pretreatment with Necrostatin-1 (Nec-1) to 92.3% and 82.9% at 1.5 h and 84.4% and 78.6% at 3.0 h, respectively. Similarly, the viability of U87 glioma cells is elevated by Necrostatin-1 to 91.6% and 81.5% at 1.5 h, and 81.8% and 71.2% at 3.0 h, respectively[3]. Necrostatin-1 (Nec-1) (30 µM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 46 mg/mL (177.38 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.3856 mL 1.9280 mL 3.8561 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Necrostatin-1 (Nec-1) is dissolved in DMSO (50 mg/mL) as stock. It is diluted in PBS before injection[5].

    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
    Molecular Weight

    259.33

    Formula

    C₁₃H₁₃N₃OS

    CAS No.

    4311-88-0

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Necrostatin-1
    Cat. No.:
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    Necrostatin-1

    Cat. No.: HY-15760