SDZ 220-040 exhibits a wide range of bioactivities across different assays and targets. It inhibits beta-lactamase AmpC with an IC50 of 160,000 nM, which increases to 220,000 nM in the presence of 0.1% Triton X-100. It also inhibits chymotrypsin with an IC50 of 270,000 nM, and this value rises to 400,000 nM in the presence of 0.1% Triton X-100. The compound has a moderate inhibitory effect on cruzain, with an IC50 of 77,000 nM, increased to 158,000 nM in the presence of 0.01% Triton X-100. It does not show significant inhibition of malate dehydrogenase (IC50 > 600,000 nM).
In addition, SDZ 220-040 demonstrates inhibitory activity against Menin-MLL interaction, HSD17B4, cytochrome P450 enzymes (2C19, 2C9), aldehyde dehydrogenase 1 (ALDH1A1), 15-hLO, ERK signaling, HPGD, GCN5L2, polymerase kappa, and vitamin D receptor (VDR), as well as USP1/UAF1. It also exhibits agonistic activity towards the Thyroid Stimulating Hormone Receptor and modulates lipid storage.
In antiviral assays, SDZ 220-040 shows activity against SARS-CoV-2 by inhibiting virus-induced cytotoxicity of Caco-2 cells with an inhibition rate of 5.78% at 10 µM after 48 hours and a 3CL-Pro protease inhibition of -13.01% at 20 µM. When tested against VERO-6 cells, it exhibits an inhibition rate of 0.16% at 10 µM after 48 hours. Additionally, it shows a modest inhibitory effect against human HDAC6 in an enzymatic assay, with a 4.67% inhibition rate using a commercial peptide substrate, but a decreased rate of -1.76% with a custom peptide substrate..
Note: Summary generated by AI. Data source: ChEMBL 