Art. -Nr.: HY-19564

JX06

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.78%
CAS. Nr.: 729-46-4
Formel: C₁₀H₁₆N₂O₂S₄
Molecular Weight:324.51

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

JX06 Chemical Structure

CAS. Nr.: 729-46-4

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	<0.5 μM Compound: JX06	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 38056298]
A549	IC₅₀	0.48 μM Compound: 16; JX06	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	[PMID: 28230989]
Kelly	IC₅₀	0.289 μM Compound: 16; JX06	Antiproliferative activity against human Kelly cells after 72 hrs by CCK8 assay Antiproliferative activity against human Kelly cells after 72 hrs by CCK8 assay	[PMID: 28230989]
L02	IC₅₀	>10 μM Compound: 16; JX06	Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay Antiproliferative activity against human LO2 cells after 72 hrs by CCK8 assay	[PMID: 28230989]

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].

MedChemExpress (MCE) 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.

In Vivo

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

MedChemExpress (MCE) 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.

Chemical Information

CAS. Nr. 729-46-4
Appearance Solid
Molecular Weight 324.51
Formel C₁₀H₁₆N₂O₂S₄
Color White to off-white
SMILES

S=C(N1CCOCC1)SSC(N2CCOCC2)=S
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

All Cell Migration/Invasion AssayIFIn Vivo Efficacy StudyWBRT-PCR

Sort by:

Journal Impact Factor

Genes Dis

2025 Nov 25.
Cell Death Dis

PRMT3 drives PD-L1-mediated immune escape through activating PDHK1-regulated glycolysis in hepatocellular carcinoma. [Abstract]

2025 Mar 6;16(1):158. PMID: 40050608

JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158. [Abstract]

Huh7 cells were infected with Lenti-PRMT3 or Lenti-Ctrl and then treated with JX06 (200 nM) or DMSO. The representative images of stained transwell chamber were shown at the right.

JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158. [Abstract]

In Huh7 xenograft mouse model, JX06 (30 mg/kg, i.p.) treatment diminished the tumor-promoting effects of PRMT3.

JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158. [Abstract]

Immunoblot analysis of PRMT3, PDHK1, and p-PDHA (phosphorylated PDHA) levels in Huh7 xenografts derived from nude mice treated with JX06 (30 mg/kg, i.p.)

JX06 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Mar 6;16(1):158. [Abstract]

PD-L1 mRNA levels were measured in Huh7 and Hepa1-6 cells with the indicated treatments. Hepatoma cells were infected with Lenti-PRMT3 or Lenti-Ctrl and then treated with JX06 (200 nM).
Int J Mol Sci

Mechanical Force Triggers Macrophage Pyroptosis and Sterile Inflammation by Disrupting Cellular Energy Metabolism. [Abstract]

2025 Apr 2;26(7):3321. PMID: 40244158

JX06 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Apr 2;26(7):3321. [Abstract]

JX06 (10 μM) significantly reduced the levels of total ROS and mitochondrial ROS in force-loaded macrophages.
BMC Musculoskelet Disord

Pyruvate Dehydrogenase Kinase 1 inhibition mediated oxidative phosphorylation enhancement in cartilage promotes osteoarthritis progression. [Abstract]

2023 Jul 20;24(1):597. PMID: 37474941
Technical University of Dresden

2025.
University of Michigan

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (154.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

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

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (538 KB)
- English - EN (538 KB)
- Français - FR (538 KB)
- Deutsch - DE (538 KB)
- Norwegian - NO (538 KB)
- Español - ES (538 KB)
- Swedish - SV (538 KB)
- Italian - IT (538 KB)
- Korean - KR (538 KB)
- Portuguese - PT (538 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0816 mL	15.4078 mL	30.8157 mL	77.0392 mL
	5 mM	0.6163 mL	3.0816 mL	6.1631 mL	15.4078 mL
	10 mM	0.3082 mL	1.5408 mL	3.0816 mL	7.7039 mL
	15 mM	0.2054 mL	1.0272 mL	2.0544 mL	5.1359 mL
	20 mM	0.1541 mL	0.7704 mL	1.5408 mL	3.8520 mL
	25 mM	0.1233 mL	0.6163 mL	1.2326 mL	3.0816 mL
	30 mM	0.1027 mL	0.5136 mL	1.0272 mL	2.5680 mL
	40 mM	0.0770 mL	0.3852 mL	0.7704 mL	1.9260 mL
	50 mM	0.0616 mL	0.3082 mL	0.6163 mL	1.5408 mL
	60 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2840 mL
	80 mM	0.0385 mL	0.1926 mL	0.3852 mL	0.9630 mL
	100 mM	0.0308 mL	0.1541 mL	0.3082 mL	0.7704 mL

Keywords

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

JX06

Apoptosis Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glycolysis Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Cysteine Targeted Covalent Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) JX06

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JX06

Apoptosis Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glycolysis Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Cysteine Targeted Covalent Library

Mitochondrial Toxicity Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) JX06

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

JX06 Related Classifications

HY-19564 Related Classifications