AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). AZ2 can be used for the research of inflammatory and immune diseases[1]. AZ2 (0.1~100 nM; 1 hour; SKOV-3 cells) excellent selectivity for PI3Kγ is further confirmed with a constitutively activated PI3K Akt pathway[1]. [1]. Gangadhara G, et al. A class of highly selective inhibitors bind to an active state of PI3Kγ. Nat Chem Biol. 2019;15(4):348-357.
AZ-2 is an inducer of ABCA1 and apoE. It enhances ABCA1 activity and decreases P2X7 receptor activity. AZ-2 activates endogenous LXR signaling but shows no direct LXRα or LXRβ agonist activity.
BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A B over CECR2 and >100-fold selectivity over all other bromodomains.