GNE684 | RIPK1 inhibitor | Probechem Biochemicals

Chemical Structure : GNE684

GNE684 (GNE-684, GNE 684)

Catalog No.: PC-49126Not For Human Use, Lab Use Only.

GNE684 (GNE 684) is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.

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Biological Activity

GNE684 (GNE 684) is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.
GNE684 inhibits necroptotic cell death in human HT-29, rat H9c2, and mouse L929 cells with EC50 of 6.6, 154 and 81 nM, respectively.
GNE684 inhibitsTNF-driven cell death effectively in several human and mouse cell lines, disrupts TBZ-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.
GNE684 inhibits RIP1 kinase driven cell death, GNE684 inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs).
GNE684 (50 mg/kg, PO, BID) reduces arthritis and skin inflammation of arthritis in paws and joints compared to wild-type mice.

Physicochemical Properties

M.Wt	432.484
Formula	C23H24N6O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-N-((S)-7-methoxy-1-methyl-2-oxo-2,3,4,5-tetrahydro-1H-pyrido[3,4-b]azepin-3-yl)-5-phenyl-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide

References

1. Snahel Patel, et al. Cell Death Differ. 2020 Jan;27(1):161-175.

GNE684 (GNE-684, GNE 684)

Biological Activity

Physicochemical Properties

References

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