GSK'872

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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)
Datasheet
Citations
Reviews (2)
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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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View all Receptor Interacting Protein Kinase Inhibitors

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

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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.

review image

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


Literature in this Area

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