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Pyridone 6

产品编号 T3080 CAS 457081-03-7

别名: Janus-Associated Kinase Inhibitor I, JAK Inhibitor, CMP 6, 吡啶酮6, JAK Inhibitor I

Pyridone 6 (JAK Inhibitor) 是一种泛JAK 抑制剂，有效抑制 JAK 激酶家族，对JAK2、TYK2、JAK3和JAK1的IC50分别为 1、1、5 和 15 nM。

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Pyridone 6, CAS 457081-03-7

规格	价格/CNY	货期
1 mg	￥ 690	现货
2 mg	￥ 995	现货
5 mg	￥ 1,490	现货
10 mg	￥ 1,980	现货
25 mg	￥ 3,360	现货
50 mg	￥ 4,890	现货
100 mg	￥ 6,980	现货
500 mg	￥ 13,900	现货
1 mL * 10 mM (in DMSO)	￥ 1,530	现货

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纯度: 98.74%

纯度: 98.7%

纯度: 98.56%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
靶点活性	JAK2:1 nM, JAK1:15 nM, TYK2:1 nM, JAK3:5 nM(Ki)
体外活性	Pyridone 6 (P6) is shown to inhibit kinase by interacting within the ATP-binding cleft of each JAK. The IC50 of Pyridone 6 is 3 nM for all of these cytokines; this is comparable to the reported IC50s of Pyridone 6 for JAK2, Tyk2, and JAK3. Pyridone 6 strongly inhibits Th2 and modestly inhibits Th1, whereas it enhances Th17 development when present within a certain range of concentrations. Pyridone 6 reduces IFN-γ and IL-13, whereas it enhances IL-17 and IL-22 expression. Pyridone 6 also inhibits both Th1 and Th2 development, whereas it promotes Th17 differentiation from naive T cells when present within a certain range of concentrations[1]. Pyridone 6 inhibits osteoclast differentiation in mouse bone marrow macrophage (BMM) cultures stimulated by the receptor activator of nuclear factor-k B (NF-k B) ligand (RANKL) and co-cultures of bone marrow cells and osteoblasts. Pyridone 6 suppresses the expression of c-Fos and nuclear factor of activated T cells (NFAT) c1 in BMMs. Pyridone 6 also suppresses I-k B degradation and extracellular signal-regulated kinase (ERK) in mature osteoclasts, suggesting that these are the key molecules that pyridone 6 targets in the inhibition of osteoclast function[2]. Pyridone 6 (P6), is found to inhibit the JAKs in the low nanomolar range (IC50, 1-15 nM) and blocks IL-2-dependent proliferation of CTLL cells. Pyridone 6 is a reversible ATP inhibitor, and when tested against many other kinases, IC50s of >130 nM are required[3].
体内活性	Pyridone 6 (P6) delays the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. P6-nano strongly ameliorates atopic dermatitis (AD) in NC/Nga mice, exerting an effect comparable to that of betamethasone ointment, a commonly used drug, which also tested as a positive control. In contrast, empty PLGA nanoparticles (C-nano) seemed to have no effect[1].
激酶实验	Kinase Assays: Baculovirus-expressed glutathione S-transferase-tagged proteins encoding the intracellular domain of IGF-1R (amino acids 957-1367) and IR (amino acids 979-1382) are used for determinations of IC50s by a homogeneous time-resolved fluorescence assay. A filter binding assay is used for appKi determinations using activated IGF-1R and IR kinases. Expanded kinase-selectivity profiling of GSK1838705A is carried out by screening the compound in the KinaseProfiler panel.
细胞实验	Pyridone 6 (P6) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1]. Naive CD4+ T cells are treated with various concentrations of Pyridone 6 in RPMI 1640 medium 1 h before the appropriate cytokines are added to create each Th-differentiating condition. Immunoblotting is performed using antiphospho-STAT protein Abs or anti-total STAT protein Abs[1].

别名	Janus-Associated Kinase Inhibitor I, JAK Inhibitor, CMP 6, 吡啶酮6, JAK Inhibitor I
分子量	309.34
分子式	C18H16FN3O
CAS No.	457081-03-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 12 mg/mL (38.79 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2327 mL	16.1634 mL	32.3269 mL	80.8172 mL
	5 mM	0.6465 mL	3.2327 mL	6.4654 mL	16.1634 mL
	10 mM	0.3233 mL	1.6163 mL	3.2327 mL	8.0817 mL
	20 mM	0.1616 mL	0.8082 mL	1.6163 mL	4.0409 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. 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. 2. Kwak HB, et al. Pyridone 6, a pan-Janus-activated kinase inhibitor, suppresses osteoclast formation and bone resorption through down-regulation of receptor activator of nuclear factor-kappaB (NF-kappaB) ligand (RANKL)-induced c-Fos and nuclear factor of a 3. Pedranzini L, et al. Pyridone 6, a pan-Janus-activated kinase inhibitor, induces growth inhibition of multiple myeloma cells. Cancer Res. 2006 Oct 1;66(19):9714-21.

文献引用

1. Li Y, Chen W, Zhu X, et al.Neuronal BST2: A Pruritic Mediator Alongside PAR2 in the Interleukin-27-Driven Itch Pathway.Journal of Investigative Dermatology.2024

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pyridone 6 457081-03-7 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Tyrosine Kinases Janus kinase Pyridone6 Pyridone-6 CMP-6 Inhibitor Janus-Associated Kinase Inhibitor I inhibit JAK Inhibitor CMP 6 吡啶酮6 CMP6 JAK Inhibitor I inhibitor

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Pyridone 6

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords