Dimercaprol demonstrates a broad spectrum of bioactivities across various biological pathways and targets. It is potent in inhibiting the splicing of Lamin A, HSD17B4 (hydroxysteroid dehydrogenase 4), Tyrosyl-DNA Phosphodiesterase (TDP1), Aldehyde Dehydrogenase 1 (ALDH1A1), HADH2 (Hydroxyacyl-Coenzyme A Dehydrogenase, Type II), GCN5L2, Histone Lysine Methyltransferase G9a, 15-hLO-2 (15-human lipoxygenase 2), Vitamin D Receptor (VDR), and Glutaminase (GLS). Additionally, it shows inhibitory effects on Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase), Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1), Human Flap endonuclease 1 (FEN1), and TGF-b. It also impacts the Cytochrome panel assay, particularly p450-cyp1a2, and impairs the function of the Influenza NS1 protein.
In cellular models, Dimercaprol has demonstrated activity against the malarial parasite plastid, Lassa Virus, Marburg Virus, and Ebola Virus, as well as in various assays related to Schwann cells. Notably, it identifies gametocytocidal compounds and has dual action in Huntington's disease models.
Furthermore, Dimercaprol inhibits NDM-1 (New Delhi metallo-beta-lactamase) with an IC50 value of 10400.0 nM using imipenem as a substrate and is involved in the activation of human PXR, leading to the induction of CYP3A4 with an efficacy of 35.5% and an EC50 value of 50100.0 nM. It exhibits competitive binding affinity to human PXR LBD and an 88.0% efficacy relative to SR12813 in a competitive binding assay.
Importantly, Dimercaprol shows no significant impact on liver toxicity parameters, with scores recorded as 0.0 for various hepatic side effects according to the Drug Induced Liver Injury Prediction System (DILIps). Additionally, it exhibits inhibitory activity against various beta-lactamases (L1, CphA, IMP1, NDM1) from Aeromonas hydrophila ATCC 7966, suggesting potential antimicrobial properties..
Note: Summary generated by AI. Data source: ChEMBL 