| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C19H17N3O2S2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK-872 is a RIPK3 inhibitor that binds the RIP3 kinase domain with an IC50 of 1.8 nM and inhibits kinase activity with an IC50 of 1.3 nM. It decreases RIPK3-mediated necroptosis and the subsequent cytoplasmic translocation and expression of HMGB1, and ameliorates brain edema and neurological deficits in early brain injury[1][2][3]. It is supplied as a white to yellow solid (C19H17N3O2S2, MW 383.49) at 99.55% purity.
Physical & Chemical Properties
| CAS Number | 1346546-69-7 |
|---|---|
| Molecular Formula | C19H17N3O2S2 |
| Molecular Weight | 383.49 g/mol |
| Purity | 99.55% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=S(C1=CC=C2N=CC=C(C2=C1)NC3=CC=C4SC=NC4=C3)(C(C)C)=O |
| Target | RIPK3 |
| Signaling Pathway | Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (260.76 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| 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. |
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 | 100 mg/mL (260.76 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
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% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (6.52 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 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). |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (6.52 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 3
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.42 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. |
Data provided by the manufacturer.
In Vitro
In human HT-29 cells, GSK-872 (GSK'872; 0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner[1].
Cell Viability Assay[1]
| Cell Line | HT-29 cells |
|---|---|
| Concentration | 0.01, 0.03, 0.1, 0.3, 1, and 3 μM |
| Incubation Time | 24 hours |
| Result | Blocked TNF-induced necroptosis in a concentration-dependent manner. |
In Vivo
GSK-872 (25 mM; intracerebroventricular injection) can attenuate brain edema, improve neurological function, and reduce the number of necrotic cells after subarachnoid hemorrhage (SAH). GSK-872 can also lower the protein levels of RIPK3 and MLKL, as well as the cytoplasmic translocation and expression of HMGB1, an important pro-inflammatory protein[3].
| Animal Model | Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)[3] |
|---|---|
| Dosage | 25 mM/6 μL |
| Administration | Syringe pump (intracerebroventricular) at 30 min after SAH |
| Result | Attenuated brain edema, improved neurological function and decreased the number of necrotic cells in the ipsilateral cortex. Decreased the expression of RIPK3, MLKL and cytoplasmic HMGB1 at 72 h after SAH in the ipsilateral cortex. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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SARS-CoV-2 triggers inflammatory responses and cell death through caspase-8 activation. Signal Transduct Target Ther 2020 Oct 9;5(1):235. PMID: 33037188
Gut stem cell necroptosis by genome instability triggers bowel inflammation. Nature 2020 Apr;580(7803):386-390.
HSPA8 acts as an amyloidase to suppress necroptosis by inhibiting and reversing functional amyloid formation. Cell Res 2023 Nov;33(11):851-866. PMID: 37580406
SARS-CoV-2 Z-RNA activates the ZBP1-RIPK3 pathway to promote virus-induced inflammatory responses. Cell Res 2023 Mar;33(3):201-214. PMID: 36650286
Expression of HIF1α in intestinal epithelium restricts arthritis inflammation by inhibiting RIPK3-induced cell death machinery. Ann Rheum Dis 2024 Mar 19:ard-2023-224491. PMID: 38503474
Mapping the holonomic signaling network that drives pathological changes in endotoxic shock. Cell Mol Immunol 2026 Jul;23(7):873-885. PMID: 42174141
Mosaic composition of RIP1-RIP3 signalling hub and its role in regulating cell death. Nat Cell Biol 2022 Apr;24(4):471-482. PMID: 35256774
RIPK1 kinase drove brain microvascular endothelial cells death and blood-brain barrier disruption in neonatal Escherichia coli meningitis. Nat Commun 2025 Aug 7;16(1):7309. PMID: 40774959
Structure-based design of potent and selective inhibitors targeting RIPK3 for eliminating on-target toxicity in vitro. Nat Commun 2025 May 8;16(1):4288. PMID: 40341069
Necroptosis enhances 'don't eat me' signal and induces macrophage extracellular traps to promote pancreatic cancer liver metastasis. Nat Commun 2024 Jul 18;15(1):6043. PMID: 39025845
