123855

AKR1C3 Inhibitor

The AKR1C3 Inhibitor controls the biological activity of AKR1C3.

• Synonym(s): AKR1C3 Inhibitor, 3-(4-(Trifluoromethyl)phenylamino)benzoic acid
• Empirical Formula (Hill Notation): C₁₄H₁₀F₃NO₂
• Molecular Weight: 281.23
• MDL number: MFCD28016823
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C(O)C1=CC(NC2=CC=C(C(F)(F)F)C=C2)=CC=C1

Description

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).

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable