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RK-24466

CAS No. : 213743-31-8

MCE 站：RK-24466

产品活性：RK-24466 (KIN 001-51) 是一种高效选择性的 Lck 抑制剂; 抑制Lck (64-509) 和LckCD亚型的IC₅₀ 值分别为小于1 和2 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src

In Vitro: RK-24466 is selective for Lck over a range of receptor, non-receptor tyrosine kinases and seronine/threonine kinases. RK-24466 are potent inhibitors of IL2 production in Jurkat cells stimulated with anti-CD3 antibody, being at least 100-fold more potent than PP1. RK-24466 displays remarkable cellular selectivity. RK-24466 significantly inhibits both VSMC proliferation and migration. RK-24466 suppresses VSMC proliferation and migration via down-regulating the protein kinase B (Akt) and extracellular signal regulated kinase (ERK) pathways, and it significantly decreases the expression of proliferating cell nuclear antigen (PCNA) and cyclin D1 and, the phosphorylation of retinoblastoma protein (pRb).

In Vivo: RK-24466 inhibits T-cell receptor stimulated (a-CD3 mAb) IL-2 production in mice at low doses (ED₅₀=4 mg/kg) after ip administration. However, efficacy is greatly reduced after oral administration (ED₅₀=25 mg/kg) which is presumed to reflect poor intestinal absorption in the latter regimen. Inhibition of antigen specific T-cell immune responses is also seen for RK-24466. After administration of RK-24466 twice daily (100 mg/kg po) for 3 days during the in vivo priming phase, a 70% inhibition of IFNγ production is seen upon subsequent antigen-specific (KLH) challenge of lymphocytes from the draining lymph nodes in vitro. RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury.

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