Brief Description

A939572 (SCD1 inhibitor) is a potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1 respectively.
IC50 value: <4 nM (mSCD1); 37 nM (hSCD1)
Target: SCD1
in vitro: A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 showed a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC50s of 65, 50, 65, and 6 nmol/L, respectively). In congruity with previous experimentation examining SCD1 lentiviral knockdown models, A939572 induced apoptosis confirmed by PARP cleavage via Western blot analysis in all 4 cell lines. InA939572 (SCDi) treated Caki1 and A498 cells, all 5 endoplasmic reticulum stress related genes were expressed at significantly increased levels compared to DMSO t BSA control, and this elevated expression could be blocked with the addition of OA-BSA.
in vivo: Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts were treated with A939572 and Tem individually or in combination over the course of 4 weeks, and tumor volume (mm3) was recorded.

Solubility

DMSO

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

White to off-white solid