GSK872

Names

[ Name ]:
GSK872

[Synonym ]:
4-Quinolinamine, N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-
N-(1,3-Benzothiazol-5-yl)-6-(isopropylsulfonyl)-4-quinolinamine
GSK'872

Biological Activity

[Description]:

GSK'872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM.

[Related Catalog]:

Signaling Pathways >> Apoptosis >> RIP kinase

Research Areas >> Inflammation/Immunology

[Target]

RIPK3[1]

[In Vitro]

GSK'872 blocks necroptosis in mouse cells. RIP3i GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis[1]. Pretreatment with GSK'872 (GSK-872) confers significant protection to primary hepatocytes. However, RIPK1 inhibition (by Nec1) does not impart any protection to primary hepatocytes[2].

[Cell Assay]

Cell viability is estimated by Trypan blue exclusion and MTT assay. Treatment of inhibitors [N-acetyl Cysteine (NAC), butylated hydroxyanisole (BHA), IM54, Bay11-7082, Z-VAD-FMK, caspase-8 inhibitor, GSK'872 (200 nM) and necrostatin-1 (Nec-1)] is given for 4 h before Deltamethrin (DLM) treatment[2].

[References]

[1]. Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95.

[2]. Arora D, et al. Deltamethrin induced RIPK3-mediated caspase-independent non-apoptotic cell death in rat primary hepatocytes. Biochem Biophys Res Commun. 2016 Oct 14;479(2):217-223.

[Related Small Molecules]

Necrostatin-1 | GSK2982772 | WEHI-345 | RIPA-56 | GSK 583 | RIP2 kinase inhibitor 1 | GSK'481 | RIP2 kinase inhibitor 2 | Nec-4

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
625.7±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₇N₃O₂S₂

[ Molecular Weight ]:
383.487

[ Flash Point ]:
332.2±31.5 °C

[ Exact Mass ]:
383.076202

[ LogP ]:
3.10

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.704

[ Storage condition ]:
-20℃