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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
ClC1=C(C(Cl)=CC=C1N2C=CN=N2)C(F)(F)F
生化/生理作用
ARUK3001185 is a brain-penetrant, orally available, potent and selective carboxylesterase Notum inhibitor (IC50 = 6.7 nM) and Wnt signaling activator with no cross-reactivity toward panels of 39 serine hydrolases, 485 kinases (IC50 >10 μM), and 47 human off-target liabilities (IC50 >30 μM).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit
Journal of medicinal chemistry, 65(10), 7212-7230 (2022)
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling
Journal of Medicinal Chemistry, 64(8), 4289-4311 (2021)
Small-molecule inhibitors of carboxylesterase Notum
Future medicinal chemistry, 13(11), 1001-1015 (2021)
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