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JX06

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纯度: 99.4%

货号 T22350Cas号 729-46-4

JX06 是一种选择性共价PDK 抑制剂,抑制PDK1,PDK2和PDK3,IC50值分别为 49 nM,101 nM 和 313 nM。它以不可逆的方式与半胱氨酸残基共价结合来抑制PDK1活性,具有抗肿瘤活性。

JX06
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JX06

一键复制产品信息
Rating icon 很棒

纯度: 99.4%

货号 T22350Cas号 729-46-4

JX06 是一种选择性共价PDK 抑制剂,抑制PDK1,PDK2和PDK3,IC50值分别为 49 nM,101 nM 和 313 nM。它以不可逆的方式与半胱氨酸残基共价结合来抑制PDK1活性,具有抗肿瘤活性。

规格价格库存数量
1 mg
¥ 159
现货
5 mg
¥ 347
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10 mg
¥ 519
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25 mg
¥ 987
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50 mg
¥ 1,670
现货
100 mg
¥ 2,650
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1 mL x 10 mM (in DMSO)
¥ 379
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产品介绍


JX06 AI Summary
JX06 exhibits a broad spectrum of bioactivities, demonstrating significant potency across various assays. It inhibits HIV-1 replication in a human T-cell line with an IC50 value of 0.52. Additionally, it inhibits human recombinant FAAH with an IC50 of approximately 79.4 µM and human MGL with an IC50 of 219 nM. The compound also shows over 50% inhibition of MGL activity at 10 µM. Beyond its antiviral activity, JX06 displays antifungal properties against Histoplasma capsulatum, with a minimum inhibitory concentration (MIC) of 40 µg/mL and efficacy in extending the survival of infected mice. Moreover, JX06 demonstrates antitrichomonas activity against Trichomonas vaginalis, with a MIC of 9.6 µM, and exhibits spermicidal activity with a minimum effective concentration of 0.1%. It also shows antifungal activity against several other fungi like Candida albicans and Cryptococcus neoformans with MIC values ranging from 38.4 µM to 76.9 µM. The compound inhibits pyruvate dehydrogenase kinases (PDKs) 1, 2, and 3, with IC50 values of 49 nM, and Ki values of 462 nM, 176 nM, and 2851 nM, respectively. It demonstrates antiproliferative effects on human A549 and Kelly cells, with IC50 values of 480 nM and 289 nM, respectively, and shows antitumor activity in A549 cell xenografts in mice. Additionally, it inhibits ALDH1A1 and ALDH2 with IC50 values of 40 nM and 1430 nM, respectively, and exhibits inhibitory effects on the SARS CoV-2 main protease (IC50 = 4030 nM) and human PHGDH (IC50 = 210 nM). JX06 also inhibits wild-type human liver FBPase by 26.08% at 10 µM. Overall, JX06 shows potential as a multi-target therapeutic agent with inhibitory activities across a range of biological targets, suggesting its applicability in treating various diseases and conditions, including infectious diseases, cancer, and metabolic disorders..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.
靶点活性
PDK1:49 nM (IC50), PDK3:313 nM (IC50), PDK2:101 nM (IC50)
化学信息
分子量324.51
分子式C10H16N2O2S4
CAS No.729-46-4
SmilesS=C(SSC(=S)N1CCOCC1)N1CCOCC1
密度1.463g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 27.5 mg/mL (84.74 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.16 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.0816 mL15.4078 mL30.8157 mL154.0785 mL
5 mM0.6163 mL3.0816 mL6.1631 mL30.8157 mL
10 mM0.3082 mL1.5408 mL3.0816 mL15.4078 mL
20 mM0.1541 mL0.7704 mL1.5408 mL7.7039 mL
50 mM0.0616 mL0.3082 mL0.6163 mL3.0816 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

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 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / 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 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 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
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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