Art. -Nr.: HY-100131

GSK481

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GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC₅₀ of 1.3 nM, which inhibits Ser¹⁶⁶ phosphorylation in wild-type human RIP1 (IC₅₀=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC₅₀ of 10 nM.

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Reinheit: 98.04%
CAS. Nr.: 1622849-58-4
Formel: C₂₁H₁₉N₃O₄
Molecular Weight:377.39

Speicherung:

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

GSK481 Chemical Structure

CAS. Nr.: 1622849-58-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1.3 nM (RIP1), 2.8 nM (Ser¹⁶⁶ phosphorylation in wild-type human RIP1)^[1]

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	>10 μM Compound: 14; GSK'481	Inhibition of mouse WT RIP1 transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA Inhibition of mouse WT RIP1 transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA	[PMID: 26854747]
HEK-293T	IC₅₀	110 nM Compound: 14; GSK'481	Inhibition of mouse RIP1 V159L mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA Inhibition of mouse RIP1 V159L mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA	[PMID: 26854747]
HEK-293T	IC₅₀	12 nM Compound: 14; GSK'481	Inhibition of mouse RIP1 V159L/T164M/Q176L/S180D/S181G mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA Inhibition of mouse RIP1 V159L/T164M/Q176L/S180D/S181G mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA	[PMID: 26854747]
HEK-293T	IC₅₀	18 nM Compound: 14; GSK'481	Inhibition of mouse RIP1 15 point mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA Inhibition of mouse RIP1 15 point mutant transfected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA	[PMID: 26854747]
HEK-293T	IC₅₀	2.8 nM Compound: 14; GSK'481	Inhibition of human WT RIP1 infected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA Inhibition of human WT RIP1 infected in HEK293T cells assessed as reduction in S166 phosphorylation by ELISA	[PMID: 26854747]
L929	IC₅₀	3.2 μM Compound: 14; GSK'481	Inhibition of mouse RIP1 in mouse L929 cells assessed as inhibition of TNF/zVAD.fmk induced necroptosis by Cell titer-Glo luminescence assay Inhibition of mouse RIP1 in mouse L929 cells assessed as inhibition of TNF/zVAD.fmk induced necroptosis by Cell titer-Glo luminescence assay	[PMID: 26854747]
U-937	IC₅₀	10 nM Compound: (S)-GSK481	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	10 nM Compound: 14; GSK'481	Inhibition of human RIP1 in human U937 cells assessed as inhibition of TNF/zVAD.fmk induced necroptosis after 24 hrs by Cell titer-Glo luminescence assay Inhibition of human RIP1 in human U937 cells assessed as inhibition of TNF/zVAD.fmk induced necroptosis after 24 hrs by Cell titer-Glo luminescence assay	[PMID: 26854747]

In Vitro

GSK481 (300 nM; 2 hours; Jurkat cells) abrogates the RIP3 up-regulation induces by both TNFa and shikonin in live and dead cells, indicating that necroptosis is in fact induced by both agents^[2].

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

Apoptosis Analysis^[2]

Cell Line:

Jurkat cells
Concentration:

300 nM
Incubation Time:

2 hours
Result:

Increased levels of detectable apoptosis induced by TNFa and shikonin.

In Vivo

GSK481 inhibits Ser¹⁶⁶ phosphorylation in three mouse RIP1 mutants (IC₅₀=18~110 nM) more potently than in wild-type mouse^[1].

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

Chemical Information

CAS. Nr. 1622849-58-4
Appearance Solid
Molecular Weight 377.39
Formel C₂₁H₁₉N₃O₄
Color Light brown to brown
SMILES

O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 35 mg/mL (92.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.6498 mL

13.2489 mL

26.4978 mL

5 mM

0.5300 mL

2.6498 mL

5.2996 mL

10 mM

0.2650 mL

1.3249 mL

2.6498 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.62 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 3

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

Solubility: ≥ 2.5 mg/mL (6.62 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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)
Handling Instructions (2659 KB)

Verweise

[1]. Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78. [Content Brief]

[2]. Lee HL, et al. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66. [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	2.6498 mL	13.2489 mL	26.4978 mL	66.2445 mL
	5 mM	0.5300 mL	2.6498 mL	5.2996 mL	13.2489 mL
	10 mM	0.2650 mL	1.3249 mL	2.6498 mL	6.6244 mL
	15 mM	0.1767 mL	0.8833 mL	1.7665 mL	4.4163 mL
	20 mM	0.1325 mL	0.6624 mL	1.3249 mL	3.3122 mL
	25 mM	0.1060 mL	0.5300 mL	1.0599 mL	2.6498 mL
	30 mM	0.0883 mL	0.4416 mL	0.8833 mL	2.2081 mL
	40 mM	0.0662 mL	0.3312 mL	0.6624 mL	1.6561 mL
	50 mM	0.0530 mL	0.2650 mL	0.5300 mL	1.3249 mL
	60 mM	0.0442 mL	0.2208 mL	0.4416 mL	1.1041 mL
	80 mM	0.0331 mL	0.1656 mL	0.3312 mL	0.8281 mL

Keywords

GSK481

1 Cited Publications

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GSK481

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Chemical Probe Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor 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

Publications Citing Use of MedChemExpress (MCE) GSK481

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK481

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Chemical Probe Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor 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

Publications Citing Use of MedChemExpress (MCE) GSK481

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK481 Related Classifications

HY-100131 Related Classifications