JX06

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JX06  纯度: 99.88%

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

JX06

JX06 Chemical Structure

CAS No. : 729-46-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥800 In-stock
25 mg ￥1800 In-stock
50 mg ￥3000 In-stock
100 mg ￥5000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JX06 相关产品

•相关化合物库:

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  • Apoptosis Compound Library
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  • Targeted Diversity Library

生物活性

JX06 is a potent, selective and covalent inhibitor of PDK. JX06 inhibits PDK1, PDK2 and PDK3 with IC50s of 49 nM, 101 nM, and 313 nM, respectively. JX06 inhibits PDK1 activity via covalently binding to a cysteine residue in an irreversible manner. JX06 shows significant antitumor activity[1].

IC50 & Target

IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)[1]
体外研究
(In Vitro)

JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM[1].
JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR[1].
JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells[1].
JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner[1].
JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells[1].
JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) [1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: A549, EBC-1, HT-29 and H460 cells
Concentration: 0, 1, 3, 10 μM
Incubation Time: 48 hours
Result: Induces cell apoptosis in A549 and EBC-1 cells.

Cell Viability Assay[1]

Cell Line: A549 cells
Concentration: 0, 0.2, 0.4, 0.6 μM
Incubation Time: 72 hours
Result: Inhibits the viability of A549 cells in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 0, 6, 12, 24 hours
Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.

体内研究
(In Vivo)

JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A549 subcutaneous xenograft mice[1]
Dosage: 40, 80 mg/kg
Administration: I.p. injections for 21 days
Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.
Well tolerated at the administration dose.

分子量

324.51

Formula

C10H16N2O2S4
CAS 号

729-46-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (154.08 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0816 mL 15.4078 mL 30.8157 mL
5 mM 0.6163 mL 3.0816 mL 6.1631 mL
10 mM 0.3082 mL 1.5408 mL 3.0816 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.70 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (7.70 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (7.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.70 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.70 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wenyi S, et, al. JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification. Cancer Res. 2015 Nov 15; 75(22): 4923-36.

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