Acid Ceramidase-IN-1 is an orally available and brain-permeable acid ceramidase (AC, ASAH-1) inhibitor.Acid Ceramidase-IN-1 can be used in the study of neurological disorders.

SABRAC inhibits acid ceramidase in PC3 MC metastatic prostate cancer cells (IC50 = <1 µM), as well as induces accumulation of ceramides in the same cells.

D-erythro-MAPP is a derivative of ceramide and an inhibitor of alkaline ceramidase (Ki = 2-13 μM; IC50 = 1-5 μM). It is selective for alkaline ceramidase over acid ceramidase (IC50 = >500 μM) as well as the serine/threonine protein phosphatase CAPP at concentrations up to 10 μM. D-erythro-MAPP increases intracellular ceramide levels, induces cell cycle arrest at the G0/G1 phase, and inhibits growth of HL-60 promyelocytic leukemia cells in a time- and concentration-dependent manner.

ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).

Acid Ceramidase-IN-2 (compound 1), an acid ceramidase inhibitor, exhibits potentially antiproliferative and cytostatic effects. This compound is of interest due to the overexpression of human acid ceramidase in prostate cancer cells, suggesting its potential anti-tumor efficacy. Furthermore, the hydrolysis of Acid Ceramidase-IN-2 can be inhibited by 3 a-ketoamides: GT85, GT98, and GT99 in vitro [1].