Dichlorisone Acetate exhibits a diverse range of bioactivities, acting as both an agonist and antagonist in various pathways. It demonstrates significant potency (5.0 nM) as both an agonist and antagonist for the Hypoxia Response Element Signaling Pathway, and functions as an inhibitor for DNA Polymerase Beta with a potency of 7943.3 nM. It also shows inhibitory effects on the Nrf2 pathway with potencies ranging from 29092.9 nM to 1299.5 nM, and on GCN5L2 with a potency of 19952.6 nM. Additionally, it induces synthetic lethality in tumor cells producing 2HG, with a potency of 4109.5 nM.
In antiviral studies, Dichlorisone Acetate has shown activity against SARS-CoV-2. It exhibits antiviral effects by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 cells at 10 µM after 48 hours, with an inhibition rate of -2.77%. It also shows 14.46% inhibition of the SARS-CoV-2 3CL-Pro protease at a concentration of 20 µM, and inhibits SARS-CoV-2 induced cytotoxicity in VERO-6 cells with an IC50 value greater than 20,000 nM.
Additionally, Dichlorisone Acetate displays binding affinity to human AR and PGR with AC50 values of 128.4 nM and 172.8 nM, respectively. It does not exhibit significant activity in inhibition assays against a variety of enzymes, and shows weak binding affinity to several receptors with AC50 values greater than 30,000 nM. However, it does exhibit antagonist activity at TBXA2R and ADRA1A, and agonist activity at HTR2B, ADRA1A, CHRM1, and TBXA2R, all with AC50 values greater than 30,000 nM. Overall, Dichlorisone Acetate interacts with a broad array of receptors and pathways, albeit with varying potency..
Note: Summary generated by AI. Data source: ChEMBL 