Pyridone 6

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Chemical Structure| 457081-03-7 同义名 : JAK Inhibitor I; CMP 6; Janus-Associated Kinase Inhibitor I; Compound 6
CAS号 : 457081-03-7
货号 : A143706
分子式 : C18H16FN3O
纯度 : 98%
分子量 : 309.34
MDL号 : MFCD06411425
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Pyridone 6 inhibits a range of 21 protein kinases with IC50s varying from 130 nM to over 10 µM. It effectively blocks IL2-driven and IL4-driven proliferation of CTLL cells with IC50s of 0.1 µM and 0.052 µM, respectively[1]. Pyridone 6 (P6) interacts with the ATP-binding cleft of JAK kinases, showing an IC50 of 3 nM for various cytokines. It strongly inhibits Th2 cell development and moderately inhibits Th1, while promoting Th17 differentiation within certain concentration ranges. P6 reduces IFN-γ and IL-13 levels but increases IL-17 and IL-22 expression, indicating its role in promoting Th17 cell differentiation from naïve T cells[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.23mL

0.65mL

0.32mL

16.16mL

3.23mL

1.62mL

32.33mL

6.47mL

3.23mL

参考文献

[1]Thompson JE, et al. Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor. Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23.

[2]Nakagawa R, et al. Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17. J Immunol. 2011 Nov 1;187(9):4611-20.