2. Apoptosis
  3. RIP kinase
  4. GSK840

GSK840 (GSK'840) est un inhibiteur de la protéine kinase 3 interagissant avec le récepteur (RIP3 ou RIPK3), qui lie le domaine kinase RIP3 avec un IC50 de 0,9 nM, et inhibe l'activité kinase avec unIC50 de 0,3 nM.

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.

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GSK840 Chemical Structure

GSK840 Chemical Structure

CAS No. : 2361146-30-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK840 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK840

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RIPK1 RIPK2 RIPK3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM[1].

IC50 & Target

IC50: 0.3 nM (RIP3)[1]
In Vitro

GSK840 (GSK'840) (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner[1].
GSK840 binds the kinase domain and inhibits kinase activity with high specificity, targeting a broader range of pro-necrotic stimuli than can be achieved with RIP1 kinase inhibitors[1].

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

GSK840 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human HT-29 cells (TNF 10 ng/ml + zVAD-fmk 20 μM + SMAC007 100 nM)
Concentration: 0.01-3 μM
Incubation Time: 24 hours
Result: Blocked TNF-induced necroptosis in a concentration-dependent manner.
Molecular Weight

365.43

Formula

C21H23N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OC(C)(C)C)CC1=CC=C(N2C3=CC=C(C(NC)=O)C=C3N=C2)C=C1
Shipping

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

DMSO : 110 mg/mL (301.02 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 2.7365 mL 13.6825 mL 27.3650 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

×
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: ≥ 2.75 mg/mL (7.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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:

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: 98.01%

SDS (251 KB)

COA (252 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
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 2.7365 mL 13.6825 mL 27.3650 mL 68.4126 mL
5 mM 0.5473 mL 2.7365 mL 5.4730 mL 13.6825 mL
10 mM 0.2737 mL 1.3683 mL 2.7365 mL 6.8413 mL
15 mM 0.1824 mL 0.9122 mL 1.8243 mL 4.5608 mL
20 mM 0.1368 mL 0.6841 mL 1.3683 mL 3.4206 mL
25 mM 0.1095 mL 0.5473 mL 1.0946 mL 2.7365 mL
30 mM 0.0912 mL 0.4561 mL 0.9122 mL 2.2804 mL
40 mM 0.0684 mL 0.3421 mL 0.6841 mL 1.7103 mL
50 mM 0.0547 mL 0.2737 mL 0.5473 mL 1.3683 mL
60 mM 0.0456 mL 0.2280 mL 0.4561 mL 1.1402 mL
80 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
100 mM 0.0274 mL 0.1368 mL 0.2737 mL 0.6841 mL
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GSK840 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:

GSK8402361146-30-5GSK'840GSK 840GSK-840RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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