| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H19N5O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK2982772 is a potent, orally active, ATP-competitive RIP1 kinase inhibitor, with IC50 values of 16 nM against human RIP1 and 20 nM against monkey RIP1[1]. It is supplied as a white to yellow solid (C20H19N5O3, MW 377.40) at 99.79% purity.
Physical & Chemical Properties
| CAS Number | 1622848-92-3 |
|---|---|
| Molecular Formula | C20H19N5O3 |
| Molecular Weight | 377.40 g/mol |
| Purity | 99.79% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(C1=NC(CC2=CC=CC=C2)=NN1)N[C@H]3COC4=CC=CC=C4N(C)C3=O |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 250 mg/mL (662.43 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: < 0.1 mg/mL (insoluble) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 250 mg/mL (662.43 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | < 0.1 mg/mL | insoluble |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Protocol 2
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.51 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 3
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.08 mg/mL (5.51 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Selectivity of GSK2982772 for ERK5 exceeds 1,000-fold over a panel of over 339 kinases at 10 μM. In cellular systems under stimulation, GSK2982772 is also able to lower spontaneous production of the cytokines IL-1β and IL-6 from ulcerative colitis explant tissue in overnight incubations, in a concentration-dependent fashion. In human embryonic kidney (HEK-293) cells, GSK2982772 weakly inhibits hERG in a concentration-dependent manner, with an estimated IC50 of 195 μM, and weakly activates the human Pregnane X receptor (hPXR), with an EC50 of 13 μM[1].
In Vivo
When dosed orally 15 min before TNF, GSK2982772 gives 68, 80, and 87% protection from temperature loss over 6 h at 3, 10, and 50 mg/kg, respectively[1]. In the matching TNF/zVAD model, protection from temperature loss over 3 h is 13, 63, and 93%. Free fraction of GSK2982772 in blood is good in rats (4.2%), dogs (11%), and cynomolgus monkeys (11%), as well as humans (7.4%)[1]. Pharmacokinetics of GSK2982772 are favorable in both rats and monkeys. It distributes into a range of tissues, including colon, liver, kidney, and heart, at concentrations comparable to those of blood[1]. Brain penetration in rat is low (4%), however, despite good cell permeability (21×10-6 cm/s)[1]. GSK2982772 itself lacks good blood-brain barrier (BBB) permeability and may enter brain tissue only under pathological conditions in which the BBB is compromised. In AAV-TAUnk01L transgenic mice (a pathological model of tauopathy in which BBB permeability is potentially increased), GSK2982772 given i.p. at 2.5 mg/kg once daily for 3 weeks can cross the compromised BBB and inhibit TAU-induced astrocyte activation; under normal physiological conditions, however, P-glycoprotein efflux impairs its BBB permeability, making brain entry difficult.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Animal Administration[1]
Mice: Use 7 mice per dose group and orally predose them with saline or GSK2982772 at 3, 10, and 50 mg/kg, 15 min before i.v. administration of mouse TNF (30 μg/mouse). Measure temperature loss with a rectal probe. End the study after 6 h, when the control group has lost 7 °C[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. Nat Commun 2026 Feb 12;17(1):1214. PMID: 41680175
RIPK3 promotes skin inflammation by enhancing IL-36α signaling and necroptosis in keratinocytes. Cell Death Dis 2025 Oct 24;16(1):759. PMID: 41136377
RIPK1 inhibitor ameliorates pulmonary injury by modulating the function of neutrophils and vascular endothelial cells. Cell Death Discov 2024 Mar 23;10(1):152. PMID: 38521771
Discovery of a 1 H-Pyrazol-3-Amine Derivative as a Novel, Selective, and Orally Available RIPK1 Inhibitor for the Treatment of Inflammatory Disease. J Med Chem 2025 Oct 23;68(20):21766-21785. PMID: 41077763
Structural and molecular characterization of a small-molecule TNF-α-TNFR1 inhibitor modulating cell death signaling. Biochem Pharmacol 2026 Apr:246:117727. PMID: 41571205
RIPK1 inhibitor ameliorates colitis by directly maintaining intestinal barrier homeostasis and regulating following IECs-immuno crosstalk. Biochem Pharmacol 2020 Feb:172:113751. PMID: 31837309
RIPK1 in Diffuse Glioma Pathology: From Prognosis Marker to Potential Therapeutic Target. Int J Mol Sci 2025 Jun 10;26(12):5555. PMID: 40565018
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. PLoS One 2024 Nov 1;19(11):e0308647. PMID: 39485774
bioRxiv. 2026 Jun 29.
