| Bioactivity | AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM. |
| Invitro | 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. AS2521780 suppresses CD3/CD28-induced Interleukin-2 (IL-2) gene transcription in Jurkat T cells and proliferation of human primary T cells. AS2521780 also suppresses concanavalin A-induced cytokine production by rat splenocytes and monkey peripheral blood mononuclear cells with similar potency[1]. |
| In Vivo | AS2521780 significantly reduces paw swelling in a dose-dependent manner in a rat model of adjuvant-induced arthritis[1]. |
| Name | AS2521780 |
| CAS | 1214726-89-2 |
| Formula | C30H41N7OS |
| Molar Mass | 547.76 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |