產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
GSK481 | 2mg 5mg 25mg | 1622849-58-4 | EY-Y0165679 |
Cas No.1622849-58-4
別名
化學(xué)名 (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide
分子式 C21H19N3O4
分子量 377.39
溶解度 DMF: 25 mg/mL,DMSO: 30 mg/mL,Ethanol: 30 mg/mL,Ethanol:PBS (pH 7.2) (1:10): 0.09 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
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
IC50: 1.3 nM for RIP1
GSK481 is a receptor interacting protein kinase 1 (RIP1) inhibitor.
The role of RIP1 kinase in tumor necrosis factor mediated inflammation has resulted in its emergence as a promising target for the treatment of multiple inflammatory diseases.
In vitro: Previous study showed that GSK481 could not only trigger an increase in biochemical activity but also exhibit great translation in the U937 cellular assay with IC50 of 10 nM. Moreover, GSK481 also showed complete specificity for RIP1 kinase against all other tested kinases when profiled over both a P33 radiolabeled assay screen. In tight-binding ADP-Glo IC50 evaluation with increasing ATP concentration, GSK481 exhibited a shift to lower potency, which was corresponding to a competitive model. In addition, GSK481 was also found to be a potent inhibitor of S166 phosphorylation in wild-type human RIP1 but was ineffective at reducing S166 phosphorylation for wild-type mouse RIP1. GSK481 was also able to more potently inhibit Ser166 phosphorylation in all three tested mouse RIP1 mutants than in wild-type mouse [1].
In vivo: So far, there is no animal in vivo data reported for GSK481.
Clinical trial: Up to now, GSK481 is still in the preclinical development stage.
關(guān)鍵字： 1622849-58-4;C21H19N3O4;GSK481;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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