CD437 is the prototypical adamantyl arotinoid of the retinoid-related molecule family that acts as a selective agonist of retinoic acid receptor (RAR)γ (Kds = 6.5 μM, 2.5 μM, and 77 nM for RARα, β, and γ, respectively). CD437 is cytotoxic to the acute myeloid leukemia cell line NB4 (EC50 = 0.17 μM), inducing DNA damage by producing DNA double strand breaks. CD437 also induces cell cycle arrest and apoptosis in various other cancer cells including melanoma, breast, non-small lung, and prostate cancer cells through RAR-dependent and -independent signaling pathways.
