AKR1C3 Inhibitor I | 2403

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.

AKR1C3 inhibitor I is 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.

2403 | AKR1C3 Inhibitor I DataSheet

Alternate Name/Synonyms: 3-(3,4-Dihydroisoquinolin2(1H)-ylsulfonyl)benzoic acid

Appearance: White solid

Formulation: N/A

CAS Number: N/A

Structure Available?: Yes

Peptide sequence: No

Salt Form: No

Molecular Formula: C₁₆H₁₅NO₄S

Molecular Weight: 317.36

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent and selective AKR1C3 inhibitor

MDL Number: N/A

PubChem CID: N/A

SMILES: O=S(C1=CC(C(O)=O)=CC=C1)(N2CCC(C=CC=C3)=C3C2)=O

InChi: InChI=1S/C16H15NO4S/c18-16(19)13-6-3-7-15(10-13)22(20,21)17-9-8-12-4-1-2-5-14(12)11-17/h1-7,10H,8-9,11H2,(H,18,19)

InChi Key: ZGVIUMKHTXKKOX-UHFFFAOYSA-N