| Hazard Information | Back Directory | [Description]
AS2553627 is a novel JAK inhibitor. AS2553627 prevents chronic rejection in rat cardiac allografts. AS2553627 potently inhibited JAK kinases but showed no inhibition of other kinases, including TCR-associated molecules. In a rat cardiac transplant model, oral administration of AS2553627 alone or co-administration with a sub-therapeutic dose of tacrolimus effectively prolonged cardiac allograft survival, suggesting the efficacy in treating acute rejection. AS2553627 may be a therapeutic candidate for the prevention of not only acute but also chronic rejection in cardiac transplantation. | [Uses]
AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants[1]. | [IC 50]
JAK1; JAK2; JAK3; Tyk2 | [References]
[1] Nakamura K, et al. AS2553627, a novel JAK inhibitor, prevents chronic rejection in rat cardiac allografts. Eur J Pharmacol. 2017 Feb 5;796:69-75. DOI:10.1016/j.ejphar.2016.12.025 |
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