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Submit ReviewGSK'872
Description: Potent and selective RIP3 kinase inhibitor
Chemical Name: N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
Purity: ≥98% (HPLC)
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
GSK'872 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK'872
| 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 for GSK'872
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.35 | 100 | |
| ethanol | 38.35 | 100 |
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 |
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Product Datasheets for GSK'872
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
If you know of a relevant reference for GSK'872, please let us know.
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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
Citations are publications that use Tocris products.
Currently there are no citations for GSK'872. 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 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.
