Art. -Nr.: HY-101760

GSK2982772

Name: GSK2982772
Brand: MedChemExpress
SKU: HY-101760
Price: 88.00 USD
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9 Cited Publications

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Based on 9 publication(s) in Google Scholar

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC₅₀ values of 16 nM and 20 nM for human and monkey RIP1, respectively.

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Reinheit: 99.79%
CAS. Nr.: 1622848-92-3
Formel: C₂₀H₁₉N₅O₃
Molecular Weight:377.40

Speicherung:

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

GSK2982772 Chemical Structure

CAS. Nr.: 1622848-92-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC₅₀ values of 16 nM and 20 nM for human and monkey RIP1, respectively^[1].

IC₅₀ & Target

IC50: 16 nM (human RIP1 FP)
IC50: 20 nM (monkey RIP1 FP)
IC50: 2 μM (rat RIP1 FP)
IC50: 2.5 μM (mouse RIP1 FP)^[1]

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	195 μM Compound: 5; GSK2982772	Inhibition of human ERG expressed in HEK293 cells Inhibition of human ERG expressed in HEK293 cells	[PMID: 28151659]
HT-29	CC₅₀	>100 μM Compound: A3; GSK2982772; GSK'772	Cytotoxicity against human HT-29 cells by Cell Titer Glo assay Cytotoxicity against human HT-29 cells by Cell Titer Glo assay	[PMID: 38309200]
HT-29	CC₅₀	>100 μM Compound: GSK'772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured for 16 to 24 hrs by Cell-titer-glo assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured for 16 to 24 hrs by Cell-titer-glo assay	[PMID: 36724216]
HT-29	CC₅₀	>50 μM Compound: 1; GSK772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33930803]
HT-29	CC₅₀	>50 μM Compound: GSK'772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay	[PMID: 36288088]
HT-29	CC₅₀	>50 μM Compound: GSK2982772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability Cytotoxicity against human HT-29 cells assessed as reduction in cell viability	[PMID: 37364415]
HT-29	CC₅₀	>50 μM Compound: GSK'772	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability Cytotoxicity against human HT-29 cells assessed as reduction in cell viability	[PMID: 35398729]
HT-29	CC₅₀	>50 μM Compound: GSK'772	Cytotoxicity against human HT-29 cells Cytotoxicity against human HT-29 cells	[PMID: 38484677]
HT-29	EC₅₀	0.0036 μM Compound: 1; GSK772	Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in human HT-29 cells assessed as inhibition of hTNFalpha/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 8 to 10 hrs by celltiter-glo luminescent cell viability assay	[PMID: 33930803]
HT-29	EC₅₀	2.78 nM Compound: GSK2982772	Anti-necroptosis activity against TSZ-induced human HT-29 cells Anti-necroptosis activity against TSZ-induced human HT-29 cells	[PMID: 38171150]
HT-29	EC₅₀	2.9 nM Compound: A3; GSK2982772; GSK'772	Anti-necroptic activity against human HT-29 cells assessed as cell viability pretreated with compound followed by TNF-alpha/Smac mimetic/Z-VAD-FMK stimulation for 16 hrs by Cell Titer Glo assay Anti-necroptic activity against human HT-29 cells assessed as cell viability pretreated with compound followed by TNF-alpha/Smac mimetic/Z-VAD-FMK stimulation for 16 hrs by Cell Titer Glo assay	[PMID: 38309200]
HT-29	EC₅₀	3.6 nM Compound: GSK'772	Anti-necroptotic activity in TSZ induced human HT-29 cells assessed as increase in cell viability pretreated with compound followed by TSZ stimulation and measured after 16 hrs by celltiter-glo luminescent cell viability assay Anti-necroptotic activity in TSZ induced human HT-29 cells assessed as increase in cell viability pretreated with compound followed by TSZ stimulation and measured after 16 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36288088]
HT-29	EC₅₀	3.6 nM Compound: GSK'772	Anti-necroptosis activity against human HT-29 cells assessed as inhibition of TSZ-induced necroptosis preincubated for 30 mins followed by compound addition and measured for 16 hrs by Cell-titer-glo assay Anti-necroptosis activity against human HT-29 cells assessed as inhibition of TSZ-induced necroptosis preincubated for 30 mins followed by compound addition and measured for 16 hrs by Cell-titer-glo assay	[PMID: 36724216]
HT-29	EC₅₀	4.1 nM Compound: GSK2982772	Anti-necroptotic activity against TSZ induced necroptosis in human HT-29 cells preincubated for 12 hrs followed by TSZ addition by CellTiter-Glo luminescent cell viability assay Anti-necroptotic activity against TSZ induced necroptosis in human HT-29 cells preincubated for 12 hrs followed by TSZ addition by CellTiter-Glo luminescent cell viability assay	[PMID: 37364415]
HT-29	EC₅₀	4.1 nM Compound: GSK'772	Anti-necroptosis activity against human HT-29 cell assessed as inhibition of TSZ-induced necroptosis by chemiluminescence assay Anti-necroptosis activity against human HT-29 cell assessed as inhibition of TSZ-induced necroptosis by chemiluminescence assay	[PMID: 38484677]
HT-29	IC₅₀	4.1 nM Compound: 6; GSK2982772	Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity Induction of necroptosis in human HT-29 cells assessed as increase in TNFalpha/AT-406/zVAD-FMK-induced LDH release preincubated with cells followed by TNFalpha/AT-406/zVAD-FMK addition measured after 16 to 20 hrs by CytoTox 96 nonradioactive cytotoxicity	[PMID: 29485864]
L929	EC₅₀	1260 nM Compound: GSK2982772	Anti-necroptosis activity against TSZ-induced mouse L929 cells Anti-necroptosis activity against TSZ-induced mouse L929 cells	[PMID: 38171150]
U-937	EC₅₀	1.27 nM Compound: GSK2982772	Anti-necroptosis activity against TSZ-induced human U-937 cells Anti-necroptosis activity against TSZ-induced human U-937 cells	[PMID: 38171150]
U-937	IC₅₀	6.3 nM Compound: GSK2982772; 40	Anti-necrotic activity in human U-937 cells Anti-necrotic activity in human U-937 cells	[PMID: 36346971]

In Vitro

GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC₅₀ of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC₅₀ of 13 μM^[1].

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

In Vivo

GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively^[1].
In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%)^[1].
GSK2982772 has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood^[1].
However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10^-6 cm/s)^[1].
GSK2982772 itself does not possess good blood-brain barrier (BBB) permeability and may only enter brain tissue under pathological conditions where the BBB is compromised^[2].
GSK2982772 (2.5 mg/kg, i.p., once daily for 3 weeks) can cross the compromised BBB in AAV-TAU^nk01L transgenic mice (a tauopathy pathological model with potentially increased BBB permeability), exerting an inhibitory effect on TAU-induced astrocyte activation; however, under normal physiological conditions, its BBB permeability is impaired due to P-glycoprotein efflux, making it difficult to enter brain tissue^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1622848-92-3
Appearance Solid
Molecular Weight 377.40
Formel C₂₀H₁₉N₅O₃
Color White to yellow
SMILES

O=C(C1=NC(CC2=CC=CC=C2)=NN1)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 (9)

All Cell Proliferation/Viability AssayCell Imaging/Staining

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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
Cell Death Dis

RIPK3 promotes skin inflammation by enhancing IL-36α signaling and necroptosis in keratinocytes. [Abstract]

2025 Oct 24;16(1):759. PMID: 41136377
Cell Death Discov

RIPK1 inhibitor ameliorates pulmonary injury by modulating the function of neutrophils and vascular endothelial cells. [Abstract]

2024 Mar 23;10(1):152. PMID: 38521771
J Med Chem

Discovery of a 1 H-Pyrazol-3-Amine Derivative as a Novel, Selective, and Orally Available RIPK1 Inhibitor for the Treatment of Inflammatory Disease. [Abstract]

2025 Oct 23;68(20):21766-21785. PMID: 41077763
Biochem Pharmacol

Structural and molecular characterization of a small-molecule TNF-α-TNFR1 inhibitor modulating cell death signaling. [Abstract]

2026 Apr:246:117727. PMID: 41571205
Biochem Pharmacol

RIPK1 inhibitor ameliorates colitis by directly maintaining intestinal barrier homeostasis and regulating following IECs-immuno crosstalk. [Abstract]

2020 Feb:172:113751. PMID: 31837309
Int J Mol Sci

RIPK1 in Diffuse Glioma Pathology: From Prognosis Marker to Potential Therapeutic Target. [Abstract]

2025 Jun 10;26(12):5555. PMID: 40565018

GSK2982772 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jun 10;26(12):5555. [Abstract]

Combined treatment of GSK2982772 (8, 16, 24, 48 nM) + cisplatin (CDDP) (5 μM) inhibits GBM cell growth.

GSK2982772 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jun 10;26(12):5555. [Abstract]

TUNEL results revealed higher levels of apoptosis induction when cells were sensitized with GSK2982772 and subsequently treated with CDDP.
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
bioRxiv

2026 Jun 29.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (662.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

2.6497 mL

13.2485 mL

26.4971 mL

5 mM

0.5299 mL

2.6497 mL

5.2994 mL

10 mM

0.2650 mL

1.3249 mL

2.6497 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 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.

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 3

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

Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

Protokoll

Animal Administration^[1]

Mice: A total of 7 mice per dose group are orally predosed with saline or GSK2982772 at doses of 3, 10, and 50 mg/kg 15 min before i.v. administration of mouse TNF (30 μg/ mouse). Temperature loss in the mice is measured by a rectal probe. The study is terminated after 6 h when the control group lost 7 °C^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 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. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261. [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	2.6497 mL	13.2485 mL	26.4971 mL	66.2427 mL
	5 mM	0.5299 mL	2.6497 mL	5.2994 mL	13.2485 mL
	10 mM	0.2650 mL	1.3249 mL	2.6497 mL	6.6243 mL
	15 mM	0.1766 mL	0.8832 mL	1.7665 mL	4.4162 mL
	20 mM	0.1325 mL	0.6624 mL	1.3249 mL	3.3121 mL
	25 mM	0.1060 mL	0.5299 mL	1.0599 mL	2.6497 mL
	30 mM	0.0883 mL	0.4416 mL	0.8832 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	0.5299 mL	1.3249 mL
	60 mM	0.0442 mL	0.2208 mL	0.4416 mL	1.1040 mL
	80 mM	0.0331 mL	0.1656 mL	0.3312 mL	0.8280 mL
	100 mM	0.0265 mL	0.1325 mL	0.2650 mL	0.6624 mL

Bioz

Keywords

GSK2982772

9 Cited Publications

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Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

GSK2982772

GSK-872

Necrostatin 2 racemate

GW806742X

Necrostatin-1

GSK840

Eclitasertib

PK68

Sorafenib

GSK547

Z-VAD-FMK

Bortezomib

Necrosulfonamide

Publications Citing Use of MedChemExpress (MCE) GSK2982772

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2982772 Related Classifications

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Bioz