Piperacetazine exhibits a diverse range of bioactivities across multiple biological targets and pathways. It shows notable inhibition potential against Menin-MLL interaction in MLL-related leukemias (potency of 25178.5 nM), Ubiquitin-specific Protease USP2a (5011.9 nM), Cytochrome P450 2D6 (199.5 nM), Chronic Active B-Cell Receptor Signaling (20596.2 nM), and 15-human lipoxygenase 2 (15-hLO-2) (12589.3 nM). Additionally, it demonstrates delayed death inhibition of the malarial parasite plastid with potencies between 5725.5 nM and 10417.9 nM, inhibition of Cell Surface uPA Generation (10000.0 nM), and induces DNA re-replication in various cell types (631.0 nM to 32642.7 nM). It also impedes Ebola Virus entry (AC50 from 2.818 µM to 9.68 µM).
In the context of SARS-CoV-2, Piperacetazine shows antiviral action, although the results vary. It inhibits SARS-CoV-2 cytotoxicity in Caco-2 cells with a modest inhibition percentage of -6.36% at 10 µM. It demonstrates inhibition against SARS-CoV-2 in HRCE cells, with moderate activity and a hit score of 0.01497, and suppresses SARS-CoV-2 3CL-Pro protease at 20 µM with an inhibition rate of -5.056%. In VERO-E6 cells, it inhibits virus-induced cytotoxicity with IC50 values ranging from 12,589.25 nM to 16,218.1 nM and demonstrates cell toxicity with a CC50 of 12,200.0 nM.
Furthermore, Piperacetazine acts as a potent inhibitor of the human HDAC6 enzyme, with significant inhibition percentages (38.43% to 77.68%) and an IC50 value of 2187.0 nM. It also presents high binding affinity towards several receptors, including HRH1, DRD2, ADRA1A, ADRA1C, DRD3, and HRH3 (AC50 from 13.0 nM to 180.0 nM), displaying both agonist (HTR2A) and antagonist (HTR2B, CNR1, HTR1A) activities, and inhibits targets like PTGS2 and PDE3A.
Despite its broad spectrum of activities, Piperacetazine has moderate liver toxicity (39.0% hepatotoxicity) but does not exhibit severe liver conditions like acute or chronic hepatitis, cirrhosis, or steatosis. It has a negative inhibition index against SARS-CoV-2 in Vero E6 cells, indicating no significant effect on cell viability in these conditions..
Note: Summary generated by AI. Data source: ChEMBL 