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> Necrostatin-1 [4311-88-0]

Necrostatin-1 [4311-88-0]

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Referencia HY-15760-1mL

embalaje : 10mM/1mL

Marca : MedChemExpress

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Descripciòn

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
HT-29 CC50
> 50 μM
Compound: 1
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by celltiter glo assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by celltiter glo assay
[PMID: 37494773]
HT-29 EC50
> 10 μM
Compound: Nec-1
Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay
Anti-necroptotic activity against TSZ-treated human HT-29 cells assessed as cell survival incubated for 4 hrs followed by fresh medium replacement without compound by CCK8 assay
[PMID: 39180479]
Jurkat EC50
0.05 μM
Compound: (+/-)-1
Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells
Inhibition of TNF-alpha-induced necroptosis in FADD-deficient human Jurkat T cells
[PMID: 18467094]
Jurkat EC50
0.49 μM
Compound: 1
Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha
Effective concentration required for inhibition of necroptosis in FADD deficient Jurkat T cells treated with TNF-alpha
[PMID: 16153840]
Jurkat EC50
0.49 μM
Compound: Nec-1
Anti-necroptic activity in TNFalpha-induced human Jurkat cells assessed as cell viability pretreated for 24 hrs followed by TNFalpha induction by Cell-titer-glo assay
Anti-necroptic activity in TNFalpha-induced human Jurkat cells assessed as cell viability pretreated for 24 hrs followed by TNFalpha induction by Cell-titer-glo assay
[PMID: 36724216]
Jurkat EC50
0.54 μM
Compound: Nec-1
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability by MTT assay
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability by MTT assay
[PMID: 38199165]
Jurkat EC50
182 nM
Compound: 1
Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells
Inhibition of endogenous RIP1 autophosphorylation in human Jurkat cells
[PMID: 18408713]
Jurkat EC50
490 nM
Compound: 1
Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells
Inhibition of cellular necroptosis in TNFalpha treated FADD deficient human Jurkat cells
[PMID: 18408713]
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.
Peso molecular

259.33

Fòrmula

C13H13N3OS
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvente y solubilidad
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.

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
Pureza y Documentación
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