AKR1C3 Inhibitor I for cell activation

A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. In repeat assays it showed an IC₅₀ of 0.013 ± 0.003 μM for AKR1C3, compared with 20.3 ± 3.8 μM against AKR1C1 and >30 μM against AKR1C2 and AKR1C4. This inhibitor also showed displays potency in a cellular assay, blocking the ability of AKR1C3 to metabolize a proven substrate. Does not display any COX (cyclooxygenase) inhibition at 10 µM in whole blood assay.

No

N/A

317.36

Biochemicals

3-(3,4-Dihydroisoquinolin2(1H)-ylsulfonyl)benzoic acid

C₁₆H₁₅NO₄S

White solid

N/A

No

Yes

≥98% by HPLC

DMSO

-20°C

gel pack

36 months

Protect from air and light

cell

For cells, cell lines and tissues in culture till half confluency.Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.