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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
NC1=C(C(NCC2=CC=C(C(NCCCC3CCCCC3)=O)C=C2)=O)C=NN1C4=CC=CC=C4
生化/生理作用
SR-318 is a potent and selective type-II inhibitor that targets p38α/β in an inactive DFG-out conformation with good kinome selectivity (p38α/β IC50 = 5/39 nM by radiometric kinase assay). SR-318 selectively inhibits p38α/β by cell-based NanoBRET assay (IC50 = 3.7 nM/p38α, 10 nM/p38β, 0.91 μM/ZAK, ≥3 μM/DDR1, DDR2, KIT, MYLK4, RSK4) and effectively blocks LPS-induced TNF-α release in human whole blood (IC50 = 283 nM). SR-321 is an inactive structural analog and the recommended negative control compound.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Journal of medicinal chemistry, 62(23), 10757-10782 (2019-11-09)
p38 mitogen-activated protein kinases are key mediators of environmental stress response and are promising targets for treatment of inflammatory diseases and cancer. Numerous efforts have led to the discovery of several potent inhibitors; however, so far no highly selective type-II
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