c82

C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.

C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.

UNC8212 is a potent TAM kinase inhibitor. It exhibits strong inhibitory activity against MERTK and AXL, with IC50 values of 1.5 nM and 1.3 nM, respectively, and also inhibits TYRO3 with an IC50 of 6.7 nM. By targeting the structurally diverse back-pocket region within the TAM kinase family, UNC8212 modulates polypharmacology characteristics. It binds tightly to TAM kinases and effectively inhibits MERTK and AXL phosphorylation. UNC8212 possesses antitumor properties and is applicable in cancer immunotherapy and target studies for tumor cells.