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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).
Catalogue Number
123855
Brand Family
Calbiochem®
Synonyms
3-(4-(Trifluoromethyl)phenylamino)benzoic acid
References
References
Adeniji, A.O., et al. 2012. J. Med. Chem.55, 2311. Adeniji, A.O., et al. 2011. Bioorg. Med. Chem. Lett. 21,1464.
AKR1C3 Inhibitor - CAS 1284180-11-5 - Calbiochem 分析证书
标题
批号
123855
参考
参考信息概述
Adeniji, A.O., et al. 2012. J. Med. Chem.55, 2311. Adeniji, A.O., et al. 2011. Bioorg. Med. Chem. Lett. 21,1464.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
27-July-2012 JSW
Synonyms
3-(4-(Trifluoromethyl)phenylamino)benzoic acid
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).
Form
White powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
1284180-11-5
Chemical formula
C₁₄H₁₀F₃NO₂
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Adeniji, A.O., et al. 2012. J. Med. Chem.55, 2311. Adeniji, A.O., et al. 2011. Bioorg. Med. Chem. Lett. 21,1464.
