acid sphingomyelinase

LCL521 inhibits lysosomal acid sphingomyelinase (ASMase).LCL521 is an acid ceramidase (ACDase) inhibitor.

Omeprazole Sodium is a proton pump inhibitor(PPI) and suppresses gastric acid secretion. Omeprazole Sodium is a potent neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor). Omeprazole Sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole Sodium inhibits growth of Gram-positive and Gram-negative bacteria.

LCL521 dihydrochloride is a dual inhibitor of acid ceramidase (ACDase) and lysosomal acid sphingomyelinase (ASMase). By targeting these lysosomal enzymes, LCL521 dihydrochloride modulates sphingolipid metabolism, with potential applications in cancer and metabolic disorder research.

ASM-IN-3 (Compound 21b) is a selective acid sphingomyelinase (ASM) inhibitor that can penetrate the blood-brain barrier, with an IC50 of 3.37 μM against purified human ASM. By inhibiting ASM activity in the hippocampus and promoting neurogenesis, ASM-IN-3 alleviates depressive-like behavior in reserpine-induced depressive rats.

BODIPY-C12 Ceramide (B12Cer) is a fluorescently-tagged form of C12 ceramide, with excitation/emission maxima at 505/540 nm, respectively. It is a fluorescently-labeled sphingolipid and has been utilized for quantifying acid sphingomyelinase activity in the plasma of patients with Niemann-Pick disease.

Drofenin is an anticonvulsant. It is an anticholinergic that acts both at the level of the nerves and the muscle fibers (neurotropic musculotropic effect). Drofenin also acts as FIASMA (functional inhibitor of acid sphingomyelinase )

ARC39 is acid sphingomyelinase inhibitor (IC50 =20 nM).

ASM-IN-1 is a potent, orally active inhibitor of acid sphingomyelinase (ASM) with an IC50 of 1.5 µM, demonstrating antiatherosclerotic and anti-inflammatory activity. It effectively reduces lipid plaques in the aortic arch and aorta, along with decreasing plasma ceramide concentrations and oxidized LDL (Ox-LDL) levels [1].

1-Aminodecylidenebis-phosphonic acid, with its potent inhibitory effect on acid sphingomyelinase (IC50= 20 nM), shows selectivity by being less effective against neutral sphingomyelinase (IC50= >100 μM). Additionally, it entirely prevents dexamethasone-induced apoptosis in HepG2 cells.

Brinazarone (SR 33287) serves as an inhibitor of acid lysosomal sphingomyelinase, subsequently causing cellular lipidosis. It enhances the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells.

2′-Hydroxy-5′-nitrohexadecanamide is an inhibitor of lysosomal hydrolase and a lipid containing pentadecanoic acid and a terminal nitrophenol group. It induces intracellular lipid accumulation by inhibiting the activity of lysosomal hydrolases. Additionally, 2′-Hydroxy-5′-nitrohexadecanamide can be used for synthesizing chromogenic substrates to assay sphingomyelinase activity.