PRT062607
Inhibitor of SYK
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
I recommend this compound as "best available" for use in cells; it is potent and cell active and almost meets a high bar for selectivity when broadly profiled. I also recommend this compound as "best available" for use in mice and rats. The original publication shows the PK data and use of the compound in in vivo models.
(last updated: 6 May 2016 )
SERP Ratings
SERP Comments:
P505-15 is a small molecule, and a potent and selective inhibitor of SYK. It inhibits SYK and suppresses BCR signaling in SUDHL4 cells and inhibits SYK-dependent signaling in human whole blood. P505-15 reversibly inhibited SYK in mice after oral dosing.
(last updated: 10 Sept 2016 )
SERP Ratings
SERP Comments:
Highly selective inhibitor of Spleen Tyrosine Kinase (SYK). Exhibits ~80-fold selectivity for SYK over the next target. Shows 1 nM potency against SYK, with substantially lower potency towards the three related kinases PTK2 (415 nM), PTK2B (108 nM), and ZAP70 (1050 nM). Potently inhibits SYK activity in cells without interfering with its activation. Potently and selectively inhibits SYK-mediated signaling in human whole blood. Orally available, with dose-dependent anti-inflammatory activity in rodent models at doses that specifically suppress SYK activity.
(last updated: 28 Apr 2017 )