SML2688
J30-8
≥98% (HPLC)
别名:
(5Z)-2-(2-Chlorophenylimino)-5-(5-fluoro-2-oxoindolin-3-ylidene)thiazolidin-4-one, 2-((2-Chlorophenyl)imino)-5-((Z)-5-fluoro-2-oxoindolin-3-ylidene)thiazolidin-4-one
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
Fc1cc2c(cc1)NC(=O)\C\2=C3/SC(=NC/3=O)Nc4c(cccc4)Cl
InChI
1S/C17H9ClFN3O2S/c18-10-3-1-2-4-12(10)21-17-22-16(24)14(25-17)13-9-7-8(19)5-6-11(9)20-15(13)23/h1-7H,(H,20,23)(H,21,22,24)/b14-13-
InChI key
HNOFQKYBQYGFNQ-YPKPFQOOSA-N
相关类别
生化/生理作用
J30-8 is a potent c-Jun N-terminal kinase JNK3 subtype-selective inhibtior (human JNK3 IC50 = 40 nM, JNK1α1 & JNK2α2 IC50 >100 μM) that exhibits excellent kinome-wide selectivity (IC50 >7.7 μM against 398 kinase targets) and neuroprotective efficacy against Aβ25-35 toxicity in SH-SY5Y cultures (1 μM). When compared with the pan-JNK inhibitor SP600125 in the APPswe/PS1dE9 murine AD model in vivo (30 mg/kg ip.), J30-8 offers superior therapeutic efficacy and pharmacokinetic properties with longer retention time (elimination t1/2 = 16.11 vs 1.23 hrs; plasma conc = 41 ng/mL vs 22 ng/mL 24 hr post ip.) and greater brain-permeability (brain/plasma ratio = 0.40 vs. 0.14 8 hr post ip.).
Potent JNK3 subtype-selective c-Jun N-terminal kinase inhibtior with superior in vivo efficacy, pharmacokinetics and brain-permeability in AD mice than SP600125.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
Xiaodong Dou et al.
Journal of medicinal chemistry, 62(14), 6645-6664 (2019-07-04)
Alzheimer's disease (AD) is one of the most challenging diseases around the world with no effective clinical treatment. Previous studies have suggested c-Jun N-terminal kinase 3 (JNK3) as an attractive therapeutic target for AD. Herein, we report 3-substituted indolin-2-one derivatives
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