Pim1 + LY333531 (Ruboxi staurin)
Pim1 + LY333531 (Ruboxi staurin): Human Pim-1 in complex with LY333531 (Ruboxistaurin)
PDB Code: 2J2I
Recently we identified LY333531 (Ruboxistaurin) as a potent inhibitor for PIM1 and PIM3 but not for PIM2. IC50s determined from enzyme kinetic assays revealed the following potencies: 200nM (PIM1), 800nM (PIM3) and 22 µM (PIM2).
LY333531 has been initially identified as a PKC-beta-specific inhibitor which reduced the development of diabetic vascular complications in animal models and prevented hyperglycemia-induced impairment of endothelial-dependent vasodilation in healthy subjects. Clinical trials showed that oral administration of LY333531 is well tolerated and ameliorates diabetes-induced retinal hemodynamic abnormalities in patients.
The observed cross reactivity of this inhibitor suggests that LY333531 might also find potential applications for the treatment of hematopoetic malignancies.
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