產(chǎn)品目錄

規(guī)格	10mM*1mLinDMSO 1mg 5mg
CAS	213743-31-8
別名	N/A
化學名	N/A
分子式	C23H22N4O
分子量	370.45
溶解度	DMSO : 45 mg/mL (121.47 mM);H2O : < 0.1 mg/mL (insoluble)
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.

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[1]. 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)[2].

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[3]. RK-24466 suppresses the migration of VSMCs from endothelium-removed aortic rings, as well as neointima formation following rat carotid balloon injury[2].

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原創(chuàng)作者：上海莼試生物技術有限公司

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