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GSK'872

Cat. No. 6492 5 Citations 1 Review Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective RIP3 kinase inhibitor
Chemical Name: N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
Purity: ≥98% (HPLC)
Datasheet
Citations (5)
Reviews (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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 and Tocriscreen Kinase Inhibitor Library. 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.

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 for GSK'872

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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

5 Citations for GSK'872

Citations are publications that use Tocris products. Selected citations for GSK'872 include:

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

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

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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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