JX06 as a selective covalent inhibitor of PDK1 in cells. JX06 dose-dependently inhibits PDK1, PDK2 and PDK3 with IC50 0.049 μM, 0.101 μM and 0.313 μM, respectively.
CAS Number: 729-46-4
Molecular Weight: 324.51
Chemical Name: Bis(morpholinothiocarbonyl) disulfide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (308.16 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM. JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR. JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells. JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner. JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells. JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .
JX06 (40-80 mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.
- 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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