A cell-permeable benzylidine-thioxothiazolidinone compound that blocks the steroidogenesis of testosterone by directly inhibiting 17b-HSD3- (17b-hydroxysteroid dehydrogenase type 3) catalyzed, NADPH-dependent, reduction of delta4-dione C17 ketone in a delta4-dione- (4-androstene-3,17-dione) competitive, highly potent (IC50=0.6, 6.0, and 40nM, respectively, against momoset, human, and mouse 17b-HSD3 activity in testes homogenate), and selective manner, displaying no activity against 17b-HSD1 and 17b-HSD2 activity. Poor pharmacokinetic properties limit its use to culture treatments and cell-free assays only.
Formula:C₁₇H₁₂BrNO₃S₂
Molecular Weight:422.3
Solubility:DMSO (50mg/ml, pinkish solution)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
