General description
A cell-permeable 3-phenyl-aminobenzoate compound that acts as a potent, competitive, reversible, active-site targeting inhibitor of aldo-keto reductase 1C3 (AKR1C3; type 5 17β-hydroxysteroid dehydrogenase) (IC50 = 60 nM) with excellent selectivity over other closely related human AKR isoforms (IC50 = 22.7, 15.4, 62.7, >50, and >50 µM for and AKR1C1, AKR1C2, AKR1C4, AKR1B1 and AKR1B10, respectively. Exhibits a weak inhibitory effect on cyclooxygenase 1 and 2 (IC50 = 100 µM). Shown to efficiently block the AKR1C3-mediated production of testosterone in LNCaP-AKR1C3 cells (~10 µM).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Adeniji, A.O., et al. 2012. J. Med. Chem.55, 2311.Adeniji, A.O., et al. 2011. Bioorg. Med. Chem. Lett.21,1464.
Packaging
25 mg in Glass bottle
Packaged under inert gas
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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