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Pyridone 6

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 Chemical Structure
Pyridone 6, CAS 457081-03-7
规格 价格/CNY 货期 数量
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
产品目录号及名称: Pyridone 6 (T3080)
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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
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 JAK3:5 nM(Ki), Tyk2:1 nM, JAK1:15 nM, JAK2:1 nM
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: 25 mg/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
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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
Tyk2-IN-3 Ruxolitinib Hypericin GTP-14564 NVP-BSK805 2HCl (1092499-93-8(free base)) Zongertinib NVP-AEW541 Ilginatinib hydrochloride

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抗癌化合物库 细胞重编程化合物库 NO PAINS 化合物库 抑制剂库 抗前列腺癌化合物库 抗肺癌化合物库 血管生成库 细胞凋亡化合物库 人代谢物化合物库

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
g
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。
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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 Tyrosine Kinases JAK 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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