Pyridone 6 (CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15nM, murine JAK1), JAK2 (IC50=1nM), JAK3 (Ki=5nM), and Tyk2 (IC50=1nM); displaying significantly weaker affinities (130nM to 10mM) for other protein tyrosine kinases.
信号通路
JAK/STAT
靶点
JAK1
JAK2
JAK3
Try2
-
IC50
15nM
1nM
5nM
1nM
-
体外研究
Pyridone 6, a pan-JAK inhibitor, delayed the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. Pyridone 6 displays potent inhibitory activity against JAK1 (IC50=15nM for murine JAK1), JAK2 (IC50=1nM), JAK3 (Ki=5nM), and Tyk2 (IC50=1nM). Pyridone 6 is therapeutic for AD by modulating the balance of Th2 and Th17. JAK inhibitor Pyridone 6 suppresses asthmatic responses by inhibiting Th2 inflammation and that application of PLGA nanoparticles improves the therapeutic potency of Pyridone 6. Inhibition of JAK may be useful for the treatment of bone-resorptive diseases, such as osteoporosis. Pyridone 6 is a more sensitive and specific inhibitor of JAK-STAT3 activity compared with AG490 and potently inhibited the growth of primary myeloma cells and myeloma-derived cell lines grown on BMSCs.
体内研究
N/A
临床实验
N/A
特征
N/A
相关实验数据(此数据来自于公开文献,信裕生物并不保证其有效性):
酶活性检测实验
方法
N/A
细胞实验
细胞系
N/A
浓度
N/A
处理时间
N/A
方法
N/A
动物实验
动物模型
N/A
配制
N/A
剂量
N/A
给药方式
N/A
参考文献: 1. Nakagawa R, Yoshida H, Asakawa M, et al. J Immunol. 2011 Nov 1, 187(9), 4611-20.
2. Yuko Matsunaga, Hiromasa Inouea, et al. Biochemical and Biophysical Research Communications. 2011, 404, 1(7), 261-267
3. Jill E. Chrencik, Akshay Patny, Iris K. Leung, et al. Journal of Molecular Biology. 2010, 400(3), 413-433.
4. Kwak HB, Kim HS, Lee MS, et al. Biol Pharm Bull. 2009 Jan, 32(1), 45-50.
5. Pedranzini L, Dechow T, Berishaj M, et al. Cancer Res. 2006 Oct 1, 66(19), 9714-21.
包装清单: