2. Membrane Transporter/Ion Channel Neuronal Signaling Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. TRP Channel Eukaryotic Initiation Factor (eIF) Reactive Oxygen Species (ROS)
  4. Necrocide 1

Necrocide 1, a necrosis by sodium overload (NECSO) inducer, is a selective transient receptor potential melastatin 4 (TRPM4) agonist with an EC50 of 306.3 nM for human TRPM4. Necrocide 1 triggers TRPM4-dependent necrotic cell death through the induction of sodium influx. Necrocide 1 induces hallmarks of immunogenic cell death incurring calreticulin (CALR) exposure, ATP secretion and high mobility group box 1 (HMGB1) release. Necrocide 1 can be used for the study of breast and prostate cancer.

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

Necrocide 1

Necrocide 1 Chemical Structure

CAS No. : 1247028-61-0

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Based on 1 publication(s) in Google Scholar

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Necrocide 1 Related Antibodies

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Description

Necrocide 1, a necrosis by sodium overload (NECSO) inducer, is a selective transient receptor potential melastatin 4 (TRPM4) agonist with an EC50 of 306.3 nM for human TRPM4. Necrocide 1 triggers TRPM4-dependent necrotic cell death through the induction of sodium influx. Necrocide 1 induces hallmarks of immunogenic cell death incurring calreticulin (CALR) exposure, ATP secretion and high mobility group box 1 (HMGB1) release. Necrocide 1 can be used for the study of breast and prostate cancer[1][2][3].

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
0.48 nM
Compound: (S)-38
Cytotoxicity against human MCF7 cells after 72 hrs by WST-1 assay
Cytotoxicity against human MCF7 cells after 72 hrs by WST-1 assay
[PMID: 20845961]
PC-3 IC50
2 nM
Compound: (S)-38
Cytotoxicity against human PC3 cells after 72 hrs by WST-1 assay
Cytotoxicity against human PC3 cells after 72 hrs by WST-1 assay
[PMID: 20845961]
In Vitro

Necrocide 1 (compound (S)-38) (72 h)shows antiproliferative activity with an IC50 value of 0.48 and 2 nM for MCF-7 and PC3, respectively[1].
Necrocide 1 (100 μM, 4-24 h) can induce phosphorylation of eIF2α in MCF-7 and A2780 cells[1].
Necrocide 1 (0.1-1000 nM, 24 h) induces necrotic cell death in various human cancer cell lines (MCF7, MB468) with species specificity, showing no effect on mouse cells due to TRPM4 differences[2].
Necrocide 1 (50-100 nM, 1-6 h) triggers massive Na+ influx, K+ efflux, membrane depolarization, and cell edema in MCF7 cells, which is blocked by TRPM4 knockout or sodium depletion[2].
Necrocide 1 (200-1000 nM, 16 h) shows increased cytotoxicity in Cos7 cells expressing gain-of-function TRPM4 mutants linked to cardiac arrhythmias, compared to wild-type TRPM4[2].
Necrocide 1 (1 μM, 0.5-1 h) specifically activates human TRPM4 (EC50 ≈ 306.3 nM) but not mouse TRPM4, as shown by patch-clamp and CETSA assays[2].
Necrocide 1 (100 nM, 3 h)-induced necrosis is inhibited by Clotrimazole (HY-10882) and dihydropyridines in MCF7 cells, blocking Na+ influx[2].
Necrocide 1 (50 nM, 4 h) induces reactive oxygen species (ROS) production in MCF-7 cells[3].
Necrocide 1 (25-100 nM, 12-48 h)-induced cell death is not inhibited by necroptosis inhibitors, ferroptosis inhibitors, pyroptosis inhibitor, or PARP inhibitor in MCF-7 and MDA-MB-468 cells[3].
Necrocide 1 (0.05-1 μM, 48 h) induces calreticulin (CALR) exposure, ATP secretion, and HMGB1 release, which are inhibited by CsA and NecroX-5 (HY-104015) in MCF-7 cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Necrocide 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 and A2780 cells
Concentration: 100 μM
Incubation Time: 4, 24 h
Result: Induced the phosphorylation of eIF2α.
In Vivo

Necrocide 1 (compound (S)-38) (20 mg/kg, i.v., on days 0 and 7) exhibits potent antitumor efficacy in PC3 rat xenograft model[1].
Necrocide 1 (40 mg/kg, i.v., on day 0, with a second injection on day 28) induces significant and sustained tumor regression in PC-3 xenografts in nude mice (effect lasting up to 20 days)[3].
Necrocide 1 (100 mg/kg, i.g., 3 times/week, 2 weeks) reduces tumor growth in PC-3 xenografts in athymic mice[3].
Necrocide 1 (30 mg/kg, i.v., 3 times/week, 2 weeks) suppresses tumor growth in MCF-7 xenografts in athymic mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC3 cells (1×107 in 200 µL PBS with 100 µL Matrigel) were subcutaneously implanted into the flanks of female nude rats (NIHRNU-M)[1]
Dosage: 20 mg/kg
Administration: i.v. on days 0 and 7
Result: Achieved complete tumor regression in PC3 rat xenograft model at a dose of 20 mg/kg.
Showed no tumor regrowth observed by day 26.
Exhibited no effect on body weights of rats.
Caused no signs of toxicity in rats.
Animal Model: PC-3 cells (1×107 in 200 µL PBS mixed with 100 µL Matrigel) were subcutaneously inoculated into female NMRI nude mice (4-5 weeks old)[3]
Dosage: 40 mg/kg
Administration: i.v. on day 0, with a second injection on day 28
Result: Induced significant tumor regression in PC-3 xenografts in nude mice at a dose of 40 mg/kg (i.v., on day 0).
Showed sustained tumor regression lasting up to 20 days before regrowth was observed.
Exhibited sensitivity of relapsed tumors to the second injection on day 28, inducing sustained regression again.
Caused no reduction in body weights of mice.
Showed no gross pathological signs in mice.
Animal Model: PC-3 cells (1×107 in 200 µL PBS mixed with 100 µL Matrigel) were subcutaneously inoculated into female NMRI nude mice (4-5 weeks old)[3]
Dosage: 100 mg/kg
Administration: i.g., 3 times/week for 2 weeks
Result: Consistently reduced PC-3 xenograft tumor growth.
Showed good tolerance in mice.
Caused no body weight reduction in mice.
Induced no gross pathological signs in mice.
Animal Model: MCF-7 cells (1×107 in 200 µL PBS mixed with 100 µL Matrigel) were subcutaneously implanted into the flanks of female NMRI nude mice (4-5 weeks old)[3]
Dosage: 30 mg/kg
Administration: i.v. 3 times/week for 2 weeks
Result: Successfully suppressed MCF-7 xenograft tumor growth.
Showed good tolerance in mice.
Caused no body weight reduction in mice.
Induced no gross pathological signs in mice.
Molecular Weight

365.47

Formula

C23H27NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(C=CC(OC)=C2C)[C@]1(C3CCCCCC3)C4=CC=C(O)C=C4
Shipping

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

DMSO : 100 mg/mL (273.62 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 2.7362 mL 13.6810 mL 27.3620 mL
5 mM 0.5472 mL 2.7362 mL 5.4724 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

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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: 2.5 mg/mL (6.84 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (6.84 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7362 mL 13.6810 mL 27.3620 mL 68.4051 mL
5 mM 0.5472 mL 2.7362 mL 5.4724 mL 13.6810 mL
10 mM 0.2736 mL 1.3681 mL 2.7362 mL 6.8405 mL
15 mM 0.1824 mL 0.9121 mL 1.8241 mL 4.5603 mL
20 mM 0.1368 mL 0.6841 mL 1.3681 mL 3.4203 mL
25 mM 0.1094 mL 0.5472 mL 1.0945 mL 2.7362 mL
30 mM 0.0912 mL 0.4560 mL 0.9121 mL 2.2802 mL
40 mM 0.0684 mL 0.3420 mL 0.6841 mL 1.7101 mL
50 mM 0.0547 mL 0.2736 mL 0.5472 mL 1.3681 mL
60 mM 0.0456 mL 0.2280 mL 0.4560 mL 1.1401 mL
80 mM 0.0342 mL 0.1710 mL 0.3420 mL 0.8551 mL
100 mM 0.0274 mL 0.1368 mL 0.2736 mL 0.6841 mL
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  • 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:

Necrocide 11247028-61-0Necrocide1Necrocide-1TRP ChannelEukaryotic Initiation Factor (eIF)Reactive Oxygen Species (ROS)Transient receptor potential channelsMCF-7PC3cancerNecroptosisCALRHMGB1Inhibitorinhibitorinhibit

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