A939572 | SCD1 inhibitor

A939572 (1032229-33-6) is a potent stearoyl-CoA desaturase 1 (SCD1) inhibitor (IC₅₀s = mouse: <4 nM, human: 37 nM).¹ Active in various cancer models alone and in combination with other chemotherapeutics.^2-6 A939572 was able to selectively eliminate human pluripotent stem cells (hPSCs) in the presence of progenitor and differentiated cells.⁷

References/Citations:

1. Xin et al. (2008), Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors; Bioorg. Med. Chem. Lett., 18 4298
2. Von Roemeling et al. (2013), Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma; Clin. Cancer Res., 19 2368
3. Piao et al. (2019), Inhibition of stearoyl CoA desaturase-1 activity suppresses tumour progression and improves prognosis in human bladder cancer; J. Cell Mol. Med., 23 2064
4. She et al. (2019), SCD1 is required for EGFR-targeting cancer therapy of lung cancer via re-activation of EGFR/PI3K/AKT signals; Cancer Cell Int., 19 103
5. Skrypek et al. (2021), Inhibition of Stearoyl-CoA Desaturase Induces the Unfolded Protein Response in Pancreatic Tumors and Suppresses Their Growth; Pancreas, 50 219
6. Hu et al. (2022), Inhibition of Stearoyl-CoA Desaturase 1 Potentiates Anti-tumor Activity of Amodiaquine in Non-small Cell Lung Cancer; Biol. Pharm. Bull., 45 438
7. Ben-David et al. (2013), Selective Elimination of Human Pluripotent Stem Cells by an Oleate Synthesis Inhibitor Discovered in a High-Throughput Screen; Cell Stem Cell, 12 P167