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Cat.No. 6492 - GSK'872 | C19H17N3O2S2 | CAS No. 1346546-69-7
Description: Potent and selective RIP3 kinase inhibitor
Chemical Name: N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
Purity: ≥98% (HPLC)

Biological Activity

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).

Technical Data

M. Wt 383.49
Formula C19H17N3O2S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1346546-69-7
PubChem ID 54674134
Smiles CC(S(=O)(C1=CC2=C(N=CC=C2NC3=CC=C4SC=NC4=C3)C=C1)=O)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

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.35 100
ethanol 38.35 100

Preparing Stock Solutions

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

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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

If you know of a relevant reference for GSK'872, please let us know.

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