ARN 14494 is a potent serine palmitoyltransferase inhibitor (SPT; IC50 = 27.3 nM). ARN 14494 inhibits synthesis of long chain ceramides and dihydroceramides in an in vitro model of Alzheimer's diease. The compound prevents the synthesis of proinflammatory cytokines and the oxidative stress-related enzymes iNOS and COX-2 in mouse primary cortical astrocytes. ARN 14494 is neuroprotective against β-amyloid 1-42 induced neurotoxicity in primary cortical neurons co-cultured with astrocytes.
ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor. With an IC50 of ~34 μM[1].
Carvone is an agonist of TRPV3 found in spearmint oil. It suppresses cell proliferation in prostate cancer cells and inhibits the growth of Dermatophagoides.
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).
ARN19689 is an effective inhibitor of human NAAA, demonstrating high potency in the low nanomolar range (IC 50 = 0.042 μM). The compound acts through a non-covalent mechanism, highlighting its ability to interact with the enzyme for inhibition.
ARN1468 (compound 5) is a highly effective orally active inhibitor of serpins. Inhibition of serpins activity by ARN1468 enables release of proteases, thereby reducing prion accumulation. ARN1468 demonstrates pronounced anti-prion effects in ScGT1 RML, ScGT1 22L, ScN2a RML, and ScN2a 22L cell lines, with EC 50 values of 8.64, 19.3, 11.2, and 6.27 μM [1].