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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).
Compound Libraries
GSK'872 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 383.49 |
| Formula | C19H17N3O2S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1346546-69-7 |
| PubChem ID | 54674134 |
| InChI Key | ZCDBTQNFAPKACC-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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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Product Datasheets
References
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
Citations for GSK'872
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Reviews for GSK'872
Average Rating: 5 (Based on 2 Reviews.)
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Effective necroptosis inhibitor.
By
JING HE on 06/28/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HT-29
Working concentration using 10 nM for different incubation time in HT-29 cells and the cell death rate was measured.
Inhibition of necroptosis with GSK872.
By
Anonymous on 09/24/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: macrophage
used to inhibit ripk3 kinase activity to block necroptosis