rn1

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA, exhibiting a broad analgesic profile [1] [2].

ARN19874 is a selective, reversible uncompetitive inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity, with an IC50 of approximately 34 μM[1].

ARN14974 is a benzoxazolone carboxamide. ARN14974 is a potent inhibitor of acid ceramidase with IC50 of 79 nM[1].

ARN14686 is an activity-based affinity probe for the detection of N-acylethanolamine acid amidase (NAAA) using click chemistry.

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].

ARN16186; ARN 16186; ARN-16186 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. This compound targets and inhibits the PI3K enzyme, which may result in the inhibition of the PI3K Akt signaling pathway and thus inhibit cell growth and induce apoptosis in susceptible tumor cell populations.

PRN1371 is a specific and potent FGFR1-4 and CSF1R inhibitor (IC50s: 0.6 1.3 4.1 19.3 8.1 nM for FGFR1 2 3 4 and CSF1R).

RN-1 dihydrochloride is an effective and selective irreversible inhibitor of lysine-specific demethylase 1 (LSD1, IC50 = 70 nM).