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GSK-872

Catalog No. T4074   CAS 1346546-69-7
Synonyms: GSK872, GSK'872, GSK2399872A

GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GSK-872 Chemical Structure
GSK-872, CAS 1346546-69-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 198.00
50 mg In stock $ 372.00
100 mg In stock $ 556.00
500 mg In stock $ 1,220.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.3%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).
Targets&IC50 RIP3K:1.8 nM
In vitro GSK872 (1 μM) has no inhibition for most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase. In HT-29 cells, GSK872 concentration-dependently blocks TNF-induced necroptosis. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK872 inhibits DAI- or TLR3-induced (RIP1-independent) death. It induces caspase activation and then induces apoptotic cell death[1].
In vivo In compared with no treatment after ischemic injury in vivo, GSK872 can significantly reduce HIF-1α expression [3].
Synonyms GSK872, GSK'872, GSK2399872A
Molecular Weight 383.49
Formula C19H17N3O2S2
CAS No. 1346546-69-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 71 mg/mL (185.1 mM)

Ethanol: 38 mg/mL (99.1 mM)

TargetMolReferences and Literature

1. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014, 56(4):481-95. 2. Kaiser WJ, et al. Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J Biol Chem. 2013 Oct 25;288(43):31268-79. 3. Yang XS, et al. Hypoxia-inducible factor-1 alpha is involved in RIP-induced necroptosis caused by in vitro and in vivo ischemic brain injury.Sci Rep. 2017 Jul 19;7(1):5818.

TargetMolCitations

1. Yang W, Liu S, Li Y, et al. Pyridoxine induces monocyte-macrophages death as specific treatment of acute myeloid leukemia. Cancer Letters. 2020 2. Xia H, Zhang Z, You F. Inhibiting ACSL1-Related Ferroptosis Restrains Murine Coronavirus Infection. Viruses. 2021, 13(12): 2383. 3. Yi Y, Gao K, Lin P, et al. Staphylococcus aureus-Induced Necroptosis Promotes Mitochondrial Damage in Goat Endometrial Epithelial Cells. Animals. 2022, 12(17): 2218. 4. Hu G, Cui Z, Chen X, et al.Suppressing Mesenchymal Stromal Cell Ferroptosis Via Targeting a Metabolism‐Epigenetics Axis Corrects their Poor Retention and Insufficient Healing Benefits in the Injured Liver Milieu.Advanced Science.2023: 2206439. 5. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 6. Li J, Liu X, Liu Y, et al.Saracatinib inhibits necroptosis and ameliorates psoriatic inflammation by targeting MLKL.Cell Death & Disease.2024, 15(2): 122.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Antidepressant Compound Library Inhibitor Library NF-κB Signaling Compound Library Anti-Breast Cancer Compound Library Anti-Ovarian Cancer Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Bioactive Compound Library

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Keywords

GSK-872 1346546-69-7 Apoptosis NF-Κb RIP kinase translocation neurological HMGB1 Receptor-interacting protein kinases brain GSK872 GSK 872 cytoplasmic deficits Inhibitor GSK'872 edema inhibit RIPK GSK2399872A inhibitor

 

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