6-Thioinosine exhibits a broad spectrum of bioactivities, including significant inhibitory effects on both sensitive (IC50 = 10.0 nM) and multidrug-resistant (IC50 = 68.0 nM) L1210 leukemia cells, with an IC50 ratio indicating greater sensitivity in parental cells. It shows suppression of humoral immune response in mice, varying with dose and administration timing, and achieves a tumor growth inhibition rate of 150.0% in L1210 cell mice models at a single dose of 173 mg/kg. The compound is also antiviral, with virus ratings of 0.8 for HSV-1, 1.1 for VV, and 1.2 for para 3, and an in vitro toxicity threshold of 1000 ug/mL in African green monkey kidney cells.
In addition to its anticancer and antiviral properties, 6-Thioinosine exhibits antiparasitic activity against Eimeria tenella (MEC > 20.0 mg/L) and promotes differentiation in friend erythroleukemia cells with an ID50 > 2.0 mM and a 51.0% differentiation rate at 1.0 mM. It also demonstrates antioxidant capabilities with notable DPPH, galvinoxyl, and ABTS radical scavenging activities, and protection against APPH-induced oxidative damage.
6-Thioinosine shows extensive potency in enzyme inhibition and splicing modulation, affecting targets including Fructose-1,6-bisphosphate Aldolase, Aldehyde Dehydrogenase 1, various transferases, and histone methyltransferases among others. It impacts various cellular processes, inhibiting DNA repair in HEK293T cells, Ebola, Lassa, and Marburg virus entry, and shows cytotoxic effects on various tumor cell lines and HeLa cells.
Furthermore, 6-Thioinosine demonstrates antibacterial activity against Bacillus anthracis in mouse J774A.1 cells (IC50 = 40,000 nM) and cytotoxicity against both wild type and HGPRTase-deficient mouse S49 cells, with a much higher potency in the wild type (EC50 = 250 nM) compared to the deficient cells (EC50 = 400,000 nM). Additionally, it inhibits mushroom tyrosinase with a Ki value of 8000.0 nM..
Note: Summary generated by AI. Data source: ChEMBL 