AKR1C1-IN-1

Catalog No.S0764

For research use only.

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.

AKR1C1-IN-1 Chemical Structure

CAS No. 4906-68-7

Purity & Quality Control

Choose Selective AKR1C Inhibitors

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 Research:

[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 293.11
Formula

C13H9BrO3

CAS No. 4906-68-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C2=CC(=C(C(=C2)Br)O)C(=O)O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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