DIM-3,5

DIM-3,5 refers to a series of 1,1-bis(3′-indolyl)-1-(3,5-disubstitutedphenyl)methane analogs that act as potent anticancer agents. These compounds function as dual inverse agonists of the orphan nuclear receptors NR4A1 (Nur77) and NR4A2 (Nurr1). In glioblastoma (GBM) research, DIM-3,5 analogs have demonstrated the ability to downregulate the expression of O6-methylguanine-DNA methyltransferase (MGMT), a key enzyme associated with resistance to the alkylating chemotherapy temozolomide (TMZ). By inhibiting the transcriptional regulation of MGMT mediated by NR4A1, NR4A2, and Sp1, these analogs reduce MGMT mRNA and protein levels, potentially sensitizing resistant glioblastoma phenotypes to standard-of-care treatment.

Other names

1,1-bis(3′-indolyl)-1-(3,5-disubstitutedphenyl)methane analogsbis-indole derived dual NR4A1/2 inverse agonists