| Description | AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM). |
| In vitro | AS2521780 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells and it also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency[1]. AS2521780 exerts potent inhibition of recombinant human PKCθ enzyme activity (IC50=0.48 nM). Which is more than 30-fold higher than that of other PKC isoforms. Further, AS2521780 exerts little or no inhibition on other protein kinases. |
| In vivo | AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1]. |
| Target activity | PKCα:160 nM, PKCδ:160 nM, PKCθ:0.48 nM, PKCε:18 nM |
| molecular weight | 547.76 |
| Molecular formula | C30H41N7OS |
| CAS | 1214726-89-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Fukahori H, et al. Effect of AS2521780, a novel PKCθ selective inhibitor, on T cell-mediated immunity. Eur J Pharmacol. 2014 Dec 15;745:217-22. |