GSK'872

Catalog #: 6492
5 Citations 1 Review Datasheet

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6492/10
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GSK'872 | CAS No. 1346546-69-7 | RIP Kinase Inhibitors

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Description: Potent and selective RIP3 kinase inhibitor

Chemical Name: N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine

Purity: ≥98%

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Product Details

Citations (5)

Reviews (1)

Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

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).

Technical Data

M.Wt:

383.49

Formula:

C₁₉H₁₇N₃O₂S₂

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

1346546-69-7

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.

Background References

Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL.
Kaiser et al.
J.Biol.Chem., 2013;288:31268
RIP3 induces apoptosis independent of pronecrotic kinase activity.
Mandal et al.
Mol.Cell, 2014;56:481

Product Datasheets

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Citations for GSK'872

The citations listed below are publications that use Tocris products. Selected citations for GSK'872 include:

5 Citations: Showing 1 - 5

A sense-antisense RNA interaction promotes breast cancer metastasis via regulation of NQO1 expression.
Authors: Lisa Et al.
Nat Cancer 2023;4:682-698
RIPK1 activation mediates neuroinflammation and disease progression in multiple sclerosis.
Authors: Timothy Et al.
Cell Rep 2021;35:109112
Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells.
Authors: Wulf Et al.
Cells 2021;10
Combined the SMAC mimetic and BCL2 inhibitor sensitizes neoadjuvant chemotherapy by targeting necrosome complexes in tyrosine aminoacyl-tRNA synthase-positive breast cancer.
Authors: Kyung-Min Et al.
Breast Cancer Res 2020;22:130
Lytic Cell Death Mechanisms in Human Respiratory Syncytial Virus-Infected Macrophages: Roles of Pyroptosis and Necroptosis.
Authors: Tanya A Et al.
Viruses 2020;12

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Inhibition of necroptosis with GSK872

By Anonymous on 09/24/2019

Species: Mouse

used to inhibit ripk3 kinase activity to block necroptosis

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