2. Apoptosis
  3. RIP kinase
  4. GSK963

GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.

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

GSK963 Chemical Structure

GSK963 Chemical Structure

CAS No. : 2049868-46-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 480 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK963:

GSK963 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK963

View All RIP kinase Isoform Specific Products:

View All Isoforms
RIPK1 RIPK2 RIPK3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro[1].

IC50 & Target

IC50: 29 nM (RIP1 in FP binding assay)[1].
Cellular Effect
Cell Line Type Value Description References
L929 IC50
1 nM
Compound: GSK'963; 57
Anti-necroptic activity in mouse L929 cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in mouse L929 cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
[PMID: 36346971]
L929 IC50
3.1 nM
Compound: GSK963
Anti-necroptotic activity against TNFalph/Z-VAD-FMK-induced mouse L929 cells assessed as cell viability measured after 19 to 21 hrs by CellTiter-Glo luminescent cell viability assay
Anti-necroptotic activity against TNFalph/Z-VAD-FMK-induced mouse L929 cells assessed as cell viability measured after 19 to 21 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 33964444]
Neutrophil IC50
0.9 nM
Compound: GSK'963; 57
Anti-necroptic activity in human neutrophil cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in human neutrophil cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
[PMID: 36346971]
U-937 IC50
4 nM
Compound: GSK963
Anti-necroptotic activity against TNFalph/Z-VAD-FMK-induced human U-937 cells assessed as cell viability measured after 19 to 21 hrs by CellTiter-Glo luminescent cell viability assay
Anti-necroptotic activity against TNFalph/Z-VAD-FMK-induced human U-937 cells assessed as cell viability measured after 19 to 21 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 33964444]
U-937 IC50
4 nM
Compound: GSK'963; 57
Anti-necroptic activity in human U-937 cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptic activity in human U-937 cells assessed as inhibition of TNF/zVAD induced necroptosis pretreated with compound for 30 mins followed by TNF/zVAD addition and measured after 19 to 21 hrs by celltiter-glo luminescent cell viability assay
[PMID: 36346971]
In Vitro

GSK963 is >10 000-fold selective for RIP1 over 339 other kinases, lacks measurable activity against IDO and has an inactive enantiomer, GSK962, which can be used to confirm on-target effects[1].

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

GSK963 Related Antibodies
In Vivo

GSK963 (2 mg/kg) results in a complete protection from TNF+zVAD-induced temperature loss. GSK963 (0.2 mg/kg) also shows a significant response[1].

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

Animal Model: C57BL/6 mice[1].
Dosage: 0.2 mg/kg, 2 mg/kg, 10 mg/kg.
Administration: IP once.
Result: Protected mice from TNF+zVAD-induced hypothermia.
Molecular Weight

230.31

Formula

C14H18N2O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(C)C(N1N=CC[C@H]1C2=CC=CC=C2)=O
Shipping

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

DMSO : 25 mg/mL (108.55 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 4.3420 mL 21.7099 mL 43.4197 mL
5 mM 0.8684 mL 4.3420 mL 8.6839 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (10.85 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.3420 mL 21.7099 mL 43.4197 mL 108.5493 mL
5 mM 0.8684 mL 4.3420 mL 8.6839 mL 21.7099 mL
10 mM 0.4342 mL 2.1710 mL 4.3420 mL 10.8549 mL
15 mM 0.2895 mL 1.4473 mL 2.8946 mL 7.2366 mL
20 mM 0.2171 mL 1.0855 mL 2.1710 mL 5.4275 mL
25 mM 0.1737 mL 0.8684 mL 1.7368 mL 4.3420 mL
30 mM 0.1447 mL 0.7237 mL 1.4473 mL 3.6183 mL
40 mM 0.1085 mL 0.5427 mL 1.0855 mL 2.7137 mL
50 mM 0.0868 mL 0.4342 mL 0.8684 mL 2.1710 mL
60 mM 0.0724 mL 0.3618 mL 0.7237 mL 1.8092 mL
80 mM 0.0543 mL 0.2714 mL 0.5427 mL 1.3569 mL
100 mM 0.0434 mL 0.2171 mL 0.4342 mL 1.0855 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GSK963 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:

GSK9632049868-46-2GSK 963GSK-963RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK963
Cat. No.:
HY-103028A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.