P505-15
Highly selective Syk inhibitor / P505-15 is a highly selective and potent (IC50 = 1-2 nM) inhibitor of spleen tyrosine kinase (Syk).1 It potently inhibited B cell antigen receptor-mediated B cell signaling/activation and basophil degranulation. It displayed anti-inflammatory activity in rodent models of rheumatoid arthritis. P505-15 displayed efficacy in vitro and in vivo in non-Hodgkin lymphoma and chronic lymphocytic leukemia models.2,3 It protected against toxin-induced hepatic fibrosis, associated hepatocellular injury, and hepatocarcinogenesis.4 P505-15 was also found to inhibit PINK1 (IC50 = 0.5-3 µM) in HeLa cells and dopaminergic neurons.5
Biochemicals & reagents
1370261-97-4
PRT062607; BIIB-057
1) Coffey et al. (2012), Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis; J. Pharmacol. Exp. Ther. 340 350 2) Hoellenriegel et al. (2012), Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration; Leukemia 26 1576 3) Spurgeon et al. (2013), The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia; J. Pharmacol. Exp. Ther. 344 378 4) Torres-Hernandex et al. (2019), Targeting SYK signaling in myeloid cells protects against liver fibrosis and hepatocarcinogenesis; Oncogene 38 4512 5) Rasool et al. (2024), Identification and structural characterization of small molecule inhibitors of PINK1; Sci. Rep. 14 7739
-20°C
TARGET: Kinase -- DISEASE AREA: Inflammation; CancerLiver disease