II399

II399 (24-48 hours) inhibits cellular NNMT activity in 769-P cells, with 24-hour IC₅₀ = 8.8 μM and 48-hour IC₅₀ = 2.0 μM^[1].
II399 (300 μM; 8 days) completely inhibits the viability of 786-O and Caki-1 renal cancer cells at 300 μM after 8 days^[1].

II399 (10 µM; 4 hours) inhibits NNMT and attenuates palmitic acid-induced PPARγ transactivation and target gene upregulation in AML12 hepatocytes^[3].
II399 (10 μM; 2 hours) protects AML12 hepatocytes and primary mouse hepatocytes from cholesterol-induced cytotoxicity^[4].
II399 (10 μM; 2 hours) completely rescues cholesterol-induced AMPK inhibition in cholesterol-loaded AML12 hepatocytes^[4].

II399 (compound 5a) (30 minutes) inhibits recombinant NNMT in the SAHH-coupled assay with IC₅₀ = 0.049 μM and apparent K_i = 5.9 nM^[1].
II399 (K_i 5.9 nM; IC₅₀ 49 nM; 30 minutes) is a potent inhibitor of recombinant human NNMT^[2].
II399 (> 333 μM; 10 minutes) exhibits weak ssSAHH inhibition, supporting its improved selectivity relative to SAM-dependent enzymes^[2].
II399 (0.03-62.5 μM; 5 minutes) directly binds to recombinant human SHMT2 with a K_d of 2.11 μM, and binds to RNMT with a K_d > 300 μM^[2].
II399 (50 μM; 2 hours) binds to SHMT2 and MEPCE and shows a more selective target profile than LL320 in HeLa whole-cell lysates, with 18 candidate targets^[2].
II399 (50 μM; 1 hour on ice) binds to NNMT and MEPCE by CETSA and does not thermally stabilize RNMT or DPH5 in HeLa cell lysates^[2].
II399 is a competitive NNMT inhibitor in the SAHH-coupled fluorescence assay with a K_i of 5.9 nM and >1000-fold selectivity relative to the tested methyltransferases and SAHH^[5].
II399 binds both the SAM and substrate pockets in the NNMT co-crystal structure, with a chloride ion-Asp142 distance of approximately 3 Å and a Tyr204-phenyl stacking distance of approximately 3.6 Å^[5].

II399 (30 min) binds to recombinant NNMT in the FP assay with K_i values of 0.077 and 0.072 μM^[1].
II399 binds to hNNMT with K_d = 336 nM^[1].
The PAMPA permeability of II399 (200 μM; 5 hours) is 0.3 × 10^-6 cm/s^[1].
II399 inhibits NNMT in FP competition assays with a K_i of 77 nM^[5].
II399 binds to NNMT as determined by ITC, with a K_d of 336 nM^[5].
II399 (1 μM; 5 hours) is cell-permeable, and an intracellular concentration of 1 μM is detected in cells after 5 hours^[5].
II399 (24-48 hours) reduces cellular MNA, with an IC₅₀ of 7.9 μM at 24 hours and 1.9 μM at 48 hours in cells, representing a cell-active NNMT bisubstrate inhibitor^[5].