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。

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.

Solid

IC50: 49 nM (PDK1), 101 nM (PDK2), 313 nM (PDK3)

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) . has not independently confirmed the accuracy of these methods. They are for reference only.

JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: A549 subcutaneous xenograft mice

Room temperature in continental US; may vary elsewhere.

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

[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.

In Vitro: DMSO : 50 mg/mL (154.08 mM; Need ultrasonic)配制储备液