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。
| 生物活性 | JX06 is a potent, selective and covalent inhibitor ofPDK. JX06 inhibitsPDK1,PDK2andPDK3withIC50s 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].
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].
| 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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
|
