AS-605240
PI 3-Kinase inhibitor / Potent and selective inhibitor of PI 3-kinase (PI 3-K ), IC50 = 8 nM displaying 30-fold selectivity over PI 3-K and PI 3-K and 7.5-fold selectivity over PI 3-Kα1. Suppresses joint inflammation in two distinct mouse models1. Ameliorates surgical brain injury2, colitis3, intimal hyperplasia-induced inflammatory processes4 and renal injury/fibrosis5 in rodent models. Orally active.
Biochemicals & reagents
648450-29-7
1) Camps et al. (2005), Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis; Nature Med., 11 936 2) Huang et al. (2015), Phosphoinositide 3-Kinase Gamma Contributes to Neuroinflammation ina Rat Model of Surgical Brain Injury; J. Neurosci., 35 10390 3) Peng et al. (2010), Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice; J. Pharmacol. Exp. Ther., 332 46 4) Smimova et al. (2014), Targeting PI3K? activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response; J. Exp. Med., 211 1779 5) Yu et al. (2018), A blockade of PI3K? signaling effectively mitigates angiotensin II-induced renal injury and fibrosis in a mouse model; Sci. Rep., 8 10988
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TARGET: Kinase -- PATHWAY: PI3K -- DISEASE AREA: Inflammation