For research use only. Not Intended for Therapeutic Use!
|IC50:||<4 nM (mSCD1); 37 nM (hSCD1) |
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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) 
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 .
. Xin Z, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302.
. von Roemeling CA, et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80.