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123855

Sigma-Aldrich

AKR1C3 Inhibitor

The AKR1C3 Inhibitor controls the biological activity of AKR1C3.

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

Quality Level

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

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

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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