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GSK872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with high affinity IC50 of 1.8 nM. GSK872 inhibits TNF- and virus-induced necrosis in 3T3-SA fibroblasts. It also inhibits necrosis induced by toll-like receptor 3 (TLR3). Pretreatment with GSK872 confers significant protection to primary hepatocytes.
Poult Sci. 2024 Oct 24.
Selenomethionine alleviates kidney necroptosis and inflammation by restoring lipopolysaccharide-mediated mitochondrial dynamics imbalance via the TLR4/RIPK3/DRP1 signaling pathway in laying hens
GSK872 purchased from AbMole
Patent. US2024024368A1 2024-12-19.
Patent. US2024024368A1
GSK872 purchased from AbMole
Patent. US2024024368A1 2024 Dec 19; .
Patent. US2024024368A1
GSK872 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | CEK cells |
| Preparation method | Cytotoxicity assays for SeMet (0, 0.025, 0.05, 0.075, 0.1, and 0.15 mM), TAK242 (0, 4.0, 8.0, 12.0, 16.0, 20.0, and 24.0 μM), GSK872 (0, 0.5, 1.0, 1.5, 2.0, 2.5, and 3.0 μM) and Mdivi-1 (0, 40, 80, 100, 120, and 140 nM) were performed as described above. Finally, 0.075 mM SeMet, 16 μM TAK242, 1.5 μM GSK872, and 100 nM Mdivi-1 were selected for pretreatment of CEK cells |
| Concentrations | 0, 0.5, 1.0, 1.5, 2.0, 2.5, and 3.0 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female, BALB/c mice |
| Formulation | - |
| Dosages | 1.9 mM/kg |
| Administration | Orally |
| Molecular Weight | 383.49 |
| Formula | C19H17N3O2S2 |
| CAS Number | 1346546-69-7 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Mandal P, et al. Mol Cell. RIP3 induces apoptosis independent of pronecrotic kinase activity.
| Related RIPK Products |
|---|
| Necrostatin-1
Necrostatin-1 (NEC-1) is a potent inhibitor of necroptosis, with an EC50 of 490 nM in Jurkat cells. Necrostin-1 is the first identified RIPK1 inhibitor, EC50=182 nM, that reduces inflammation and inhibits colitis associated tumorigenesis. Necrostatin-1 (Nec-1) is also an inhibitor of IDO. |
| GSK481
GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM. |
| GSK583
GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. |
| Necrostatin-5
Necrostatin-5 is an inhibitor of necroptosis (non-apoptotic cell death pathway) by indirect inhibition of RIP1 kinase, with an EC50 value of 0.24 µM. |
| WEHI-345
WEHI-345 is a potent and selective RIPK2 inhibitor with IC50 of 0.13 μM. WEHI-345 delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation. |
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