Cat. No.: HY-103028A

GSK963

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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.

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Pureté: 99.10%
CAS No.: 2049868-46-2
Formule: C₁₄H₁₈N₂O
Masse moléculaire:230.31

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK963 Chemical Structure

CAS No.: 2049868-46-2

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 29 nM (RIP1 in FP binding assay)^[1].

Voir tous les produits spécifiques à Isoform RIP kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
BMDM	IC₅₀	3 nM Compound: 4; (S)-GSK'963	Anti-necroptotic activity in mouse BMDM cells assessed as inhibition of LPS/QVD induced necroptosis pretreated for 30 mins measured after 19 to 21 hrs by CellTiter-Glo Luminescent Cell Viability assay Anti-necroptotic activity in mouse BMDM cells assessed as inhibition of LPS/QVD induced necroptosis pretreated for 30 mins measured after 19 to 21 hrs by CellTiter-Glo Luminescent Cell Viability assay	[PMID: 36781172]
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	1 nM Compound: 4; (S)-GSK'963	Anti-necroptotic activity in mouse L929 cells assessed as inhibition of LPS/Z-VAD-fmk induced necroptosis pretreated for 30 mins measured after 19 to 21 hrs by CellTiter-Glo Luminescent Cell Viability assay Anti-necroptotic activity in mouse L929 cells assessed as inhibition of LPS/Z-VAD-fmk induced necroptosis pretreated for 30 mins measured after 19 to 21 hrs by CellTiter-Glo Luminescent Cell Viability assay	[PMID: 36781172]
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.

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.

Chemical Information

CAS No. 2049868-46-2
Appearance Solid
Masse moléculaire 230.31
Formule C₁₄H₁₈N₂O
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Pharmacol Rep

An in vitro evaluation of the antioxidant activities of necroptosis and apoptosis inhibitors: the potential of necrostatin-1 and necrostatin-1i to have radical scavenging activities. [Abstract]

2023 Apr;75(2):490-497. PMID: 36719636

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3420 mL

21.7099 mL

43.4197 mL

5 mM

0.8684 mL

4.3420 mL

8.6839 mL

10 mM

0.4342 mL

2.1710 mL

4.3420 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Berger SB, et al. Characterization of GSK'963: a structurally distinct, potent and selective inhibitor of RIP1 kinase. Cell Death Discov. 2015 Jul 27;1:15009. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

GSK963

1 Cited Publications

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GSK963

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) GSK963

Voir tous les produits spécifiques à Isoform RIP kinase

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK963

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) GSK963

Voir tous les produits spécifiques à Isoform RIP kinase

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GSK963 Related Classifications

HY-103028A Related Classifications