An orally bioavilable diacetyloxy-naphthoquinone compound that directly targets insulin receptor tyrosine kinase (IRTK) domain and specifically increases IR kinase activity with no effect on IGF-1R and EGFR. Shown to rapidly phosphorylate IR (Tyr1146 and Tyr1158/1162/1163) and IRS-1 and selectively activate insulin signaling Akt (Thr473) and ERK pathways in CHO-IGF-IR cells at 5uM. Sensitizes insulin action, enhances glucose uptake in differentiated 3T3-L1 adipocytes and decreases blood glucose levels in both normal and diabetic C57BL/6J mice (20mg/kg, p.o.).
Formula:C14H8Cl2O6
Molecular Weight:343.1
Solubility:DMSO (25mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
