1. Metabolic Enzyme/Protease
    Apoptosis
  2. PDHK
    Apoptosis
  3. JX06

JX06 

Cat. No.: HY-19564
Handling Instructions

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.

For research use only. We do not sell to patients.

JX06 Chemical Structure

JX06 Chemical Structure

CAS No. : 729-46-4

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Description

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]

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.
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.
Molecular Weight

324.51

Formula

C₁₀H₁₆N₂O₂S₄

CAS No.

729-46-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

JX06JX 06JX-06PDHKApoptosisPyruvate dehydrogenase kinasePDH kinasePDKPDK1PDK2PDK3cancerInhibitorinhibitorinhibit

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