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).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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