Home Immunology & Inflammation AKR1C inhibitor - Dehydrogenase inhibitor AKR1C1-IN-1 For research use only.

AKR1C1-IN-1

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

AKR1C1-IN-1 Chemical Structure

CAS: 4906-68-7

Purity & Quality Control

Batch: S076401 DMSO] 59 mg/mL] false] Ethanol] 59 mg/mL] false] Water] Insoluble] false Purity: 98.71%
98.71

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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
In vitro

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

Chemical Information & Solubility

Molecular Weight 293.11 Formula

C13H9BrO3
CAS No. 4906-68-7 SDF --
Smiles C1=CC=C(C=C1)C2=CC(=C(C(=C2)Br)O)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 59 mg/mL ( (201.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 59 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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