GSK'872

Catalog No.S8465 Batch:S846501

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Technical Data

Formula

C19H17N3O2S2
Molecular Weight 383.49 CAS No. 1346546-69-7
Solubility (25°C)* In vitro DMSO 76 mg/mL (198.17 mM)
Ethanol 40 mg/mL (104.3 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GSK'872 is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
Targets
RIP3K [1]
(Cell-free assay)
1.3 nM
In vitro When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death[1].
In vivo GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo[3].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    3T3-SA cells

  • Concentrations

    0.3, 1, 3 μM

  • Incubation Time

    18 h

  • Method

    Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872 are assayed.
Animal Study:

[3]
  • Animal Models

    C57BL/6 mice

  • Dosages

    1.9 mmol/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 46(2):699-712]

Selleck's GSK'872 has been cited by 67 publications

EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death [ Nat Commun, 2024, 15(1):1282] PubMed: 38346956
Heterogeneous ferroptosis susceptibility of macrophages caused by focal iron overload exacerbates rheumatoid arthritis [ Redox Biol, 2024, 69:103008] PubMed: 38142586
NR4A1 depletion inhibits colorectal cancer progression by promoting necroptosis via the RIG-I-like receptor pathway [ Cancer Lett, 2024, 585:216693] PubMed: 38301909
Bacillus cereus cereolysin O induces pyroptosis in an undecapeptide-dependent manner [ Cell Death Discov, 2024, 10(1):122] PubMed: 38458999
Role of the RIP3-PGAM5-Drp1 pathway in aluminum-induced PC12 cells necroptosis [ Ecotoxicol Environ Saf, 2024, 270:115860] PubMed: 38142589
Cooperative sensing of mitochondrial DNA by ZBP1 and cGAS promotes cardiotoxicity [ Cell, 2023, 186(14):3013-3032.e22] PubMed: 37352855
The transcription factor ATF3 switches cell death from apoptosis to necroptosis in hepatic steatosis in male mice [ Nat Commun, 2023, 14(1):167] PubMed: 36690638
Dimethyl fumarate inhibits necroptosis and alleviates systemic inflammatory response syndrome by blocking the RIPK1-RIPK3-MLKL axis [ Pharmacol Res, 2023, 189:106697] PubMed: 36796462
Fighting cancer by triggering non-canonical mitochondrial permeability transition-driven necrosis through reactive oxygen species induction [ Free Radic Biol Med, 2023, 202:35-45] PubMed: 36963639
Celastrol inhibits necroptosis by attenuating the RIPK1/RIPK3/MLKL pathway and confers protection against acute pancreatitis in mice [ Int Immunopharmacol, 2023, 117:109974] PubMed: 37012867

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.