13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg |
| CAS | 84 |
| 別名 |
|
| 化學名 | 6-(2,6-dimethylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)benzo[4,5]imidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one |
| 分子式 | C31H30N8O |
| 分子量 | 530.62 |
| 溶解度 | DMF: 12 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 2.5 mg/ml,Ethanol: 0.33 mg/ml |
| 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 |
產品描述：
Lck Inhibitor is a small-molecule inhibitor of with IC50 value of 7 nM [1].
The lymphocyte specific kinase which expressed in NK cells and T-cells is a member of the Src kinase family. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. Therefore small-molecule inhibitors of Lck with potent activities and bioavailable efficacies have been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection [1].
Lck Inhibitor showed high selectivity against Lck over another Src family kinase Src and the kinases related to inflammation and angiogenesis such as p38 and VEGFR-2 with IC50 values of 0.12, > 10 and 5.1 μM, respectively. Lck Inhibitor also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family. In cultured human mixed lymphocytes, the inhibitor significantly suppressed the activation of T-cells with IC50 value of 47 nM. Besides that, this compound inhibited IL-2 secretion induced by T-cell receptor with IC50 value of 0.46 μM. The good potency and selectivity of the Lck Inhibitor were due to the critical aniline side chain within a N-methylpiperazine moiety. It extended to the ATP-binding pocket of the enzyme and formed hydrogen bond interactions with the linker region [1].
In rats model with arthritis induced by the injection of porcine type II collagen, oral administration of the compound dose-dependently suppressed the inflammation with ED50 value of 3.2 mg/kg. While in the adjuvant-induced arthritis model, oral administration of Lck Inhibitor also displayed significant anti- arthritis effects with ED50 value of 24 mg/kg [1].
特別提醒：
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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