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Biological Activity for GSK'872
GSK'872 is a potent and selective receptor activating protein kinase 3 (RIP3) inhibitor (IC50 = 1.3 nM). Exhibits >1000-fold selectivity for RIP3 over a panel of 300 other kinases including RIP1. Inhibits TNF-induced cell death in 3T3-SA cells and TLR3-induced necrosis in fibroblasts in vitro. Blocks necroptosis of primary human neutrophils from whole blood. Also induces apoptosis at higher concentrations (3 - 10 μM).
Compound Libraries for GSK'872
Technical Data for GSK'872
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK'872
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GSK'872
The following data is based on the product molecular weight 383.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.61 mL||13.04 mL||26.08 mL|
|5 mM||0.52 mL||2.61 mL||5.22 mL|
|10 mM||0.26 mL||1.3 mL||2.61 mL|
|50 mM||0.05 mL||0.26 mL||0.52 mL|
References for GSK'872
References are publications that support the biological activity of the product.
Kaiser et al (2013) Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J.Biol.Chem. 288 31268 PMID: 24019532
Mandal et al (2014) RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol.Cell 56 481 PMID: 25459880
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Keywords: GSK'872, GSK'872 supplier, GSK872, potent, selective, receptor, activating, protein, kinase, 3, RIP3K, inhibitors, inhibits, necroptosis, necrosis, RIPK3, Necroptosis, RIP, Kinases, 6492, Tocris Bioscience
5 Citations for GSK'872
Citations are publications that use Tocris products. Selected citations for GSK'872 include:
Timothy et al (2021) RIPK1 activation mediates neuroinflammation and disease progression in multiple sclerosis. Cell Rep 35 109112 PMID: 33979622
Wulf et al (2021) Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells. Cells 10 PMID: 34831323
Tanya A et al (2020) Lytic Cell Death Mechanisms in Human Respiratory Syncytial Virus-Infected Macrophages: Roles of Pyroptosis and Necroptosis. Viruses 12 PMID: 32854254
Kyung-Min et al (2020) Combined the SMAC mimetic and BCL2 inhibitor sensitizes neoadjuvant chemotherapy by targeting necrosome complexes in tyrosine aminoacyl-tRNA synthase-positive breast cancer. Breast Cancer Res 22 130 PMID: 33239070
Lisa et al (2023) A sense-antisense RNA interaction promotes breast cancer metastasis via regulation of NQO1 expression. Nat Cancer 4 682-698 PMID: 37169843
Do you know of a great paper that uses GSK'872 from Tocris? Please let us know.
Reviews for GSK'872
Average Rating: 5 (Based on 1 Review.)
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