hA2A/hCA XII modulator 1

hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

hA2AAR:6.4 nM (Ki)

hA1AR:4.819 μM (Ki)

hA3:>30 μM (Ki)

[1]. Costanza Ceni, et al.  Discovery of first-in-class multi-target adenosine A 2A receptor antagonists-carbonic anhydrase IX and XII inhibitors. 8-Amino-6-aryl-2-phenyl-1,2,4-triazolo [4,3-a]pyrazin-3-one derivatives as new potential antitumor agents. Eur J Med Chem. 2020 Sep 1;201:112478.