RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.RIPA-56 is a type III kinase inhibitor with stable metabolism. By locking RIP1 in the inactive form, it targets receptor-interacting protein-1 kinase (RIP1; RIPK1) in a
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of receptor interacting serine/threonine kinase 1
Product Description
Information
RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor.
Targets
RIP1 (Cell-free) 13 nM
In vitro
RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM. It showed no inhibition of RIP3 kinase activity at a 10 µM concentration. RIPA-56 does not inhibit IDO activity at a concentration of 200 µM, which represents an estimated 10,000-fold selectivity window based on the RIP1 ADP-Glo activity of 13 nM.
In vivo
RIPA-56 has an impressive PK profile in mice, with a 3.1 h half-life, 22% oral bioavailability (PO), and 100% bioavailability from intraperitoneal injection (IP). RIPA-56 has great ability in transporting across blood brain barrier. In the SIRS mice disease model, RIPA-56 efficiently reduced tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage.
1.Ren Y, Su Y, Sun L, He S, Meng L, Liao D, Liu X, Ma Y, Liu C, Li S et al.. (2017) Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.. J Med Chem, 60 (3):(972-986). [PMID:27992216][10.1021/op500134e]
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F2306493