[CAS NO. 729-46-4] JX06
PRODUCTS SPECIFICATIONS [729-46-4]
DESCRIPTION [729-46-4]
Overview
| MDL | MFCD00072237 |
|---|---|
| Molecular Weight | 324.51 |
| Molecular Formula | C10H16N2O2S4 |
| SMILES | S=C(N1CCOCC1)SSC(N2CCOCC2)=S |
Summary
JX06 is a potent, selective and covalent inhibitor of PDK . JX06 inhibits PDK1 , PDK2 and PDK3 with IC 50 s 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]
.
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] .
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 154.08 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
Synonyms