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Merck

123855

AKR1C3 Inhibitor

The AKR1C3 Inhibitor controls the biological activity of AKR1C3.

Synonym(s):

3-(4-(Trifluoromethyl)phenylamino)benzoic acid, AKR1C3 Inhibitor

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About This Item

CAS Number:
1284180-11-5
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, protect from light

Key Documents

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InChI key

MDZIRNPRVJEHHX-UHFFFAOYSA-N

InChI

1S/C14H10F3NO2/c15-14(16,17)10-4-6-11(7-5-10)18-12-3-1-2-9(8-12)13(19)20/h1-8,18H,(H,19,20)

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

Quality Level

100

Related Categories

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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