AKR1C1-IN-1

Catalog No.S0764 Batch:S076401

Technical Data

Formula	C₁₃H₉BrO₃
Molecular Weight	293.11	CAS No.	4906-68-7
Solubility (25°C)*	In vitro	DMSO	59 mg/mL (201.28 mM)
		Ethanol	59 mg/mL (201.28 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

AKR1C1-IN-1 is a potent and selective inhibitor of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) with Ki of 4 nM, 87 nM, 4.2 μM and 18.2 μM for AKR1C1, AKR1C2, AKR1C3 and AKR1C4, respectively.

Targets

AKR1C1 ^[1] (Cell-free assay)	AKR1C2 ^[1] (Cell-free assay)	AKR1C3 ^[1] (Cell-free assay)	AKR1C4 ^[1] (Cell-free assay)
4 nM(Ki)	87 nM(Ki)	4.2 μM(Ki)	18.2 μM(Ki)

In vitro

AKR1C1-IN-1 significantly decreases the metabolism of progesterone in the cells with an IC50 value of 460 nM.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Bovine aortic endothelial cells Concentrations 10 µM Incubation Time 2 h Method The transfected cells were maintained in the medium containing 2% fetal bovine serum for 24 h and then used to evaluate the inhibitory effects of 3,5-dibromosalicylic acid and Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) on the metabolism of progesterone in the cells. The cells were pretreated for 2 h with various concentrations of inhibitors in serum-free growth medium prior to incubating for 6 h with 30 µM progesterone. The culture media were collected by centrifugation, and the lipidic fraction of the media was extracted twice by ethyl acetate. The metabolite, 20R-hydroxyprogesterone, was quantified on a LC-MS.

Cell Assay:^{^[1]}

Cell lines
Bovine aortic endothelial cells
Concentrations
10 µM
Incubation Time
2 h
Method
The transfected cells were maintained in the medium containing 2% fetal bovine serum for 24 h and then used to evaluate the inhibitory effects of 3,5-dibromosalicylic acid and Bisindolylmaleimide IV (Arcyriarubin A, BIM IV, Compound 5/1a) on the metabolism of progesterone in the cells. The cells were pretreated for 2 h with various concentrations of inhibitors in serum-free growth medium prior to incubating for 6 h with 30 µM progesterone. The culture media were collected by centrifugation, and the lipidic fraction of the media was extracted twice by ethyl acetate. The metabolite, 20R-hydroxyprogesterone, was quantified on a LC-MS.

References

[1] Ossama El-Kabbani, et al. J Med Chem. 2009 May 28;52(10):3259-64.

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