11-Hydroxysugiol regulates the SUMOylation of intracellular receptors by modulating RARα and vitamin D3 receptor (VDR).

Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity.

AGN 196996 (IRX6696) is a potent selective RARα antagonist with Ki of 2 nM, shows little to no activity against RARβ and RARγ.

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

CD666 is a potent, selective RARgamma (RARγ) agonist.

E6060 is a potent, selective retinoic acid receptor subtype α (RAR-α) agonist with Ki of 0.2 nM, IC50 of 0.2 nM for RAR-α-mediated reporter transactivation assays.

IRX4647 is a selective RARγ agonist, regulates T cell biology and reduces syngeneic tumor growth of immune checkpoint-resistant lung cancer cell line (344SQ) when combined with anti-PD-L1.

LG101506 (LG1506) is a potent, selective and orally active RXR modulator with Ki of 2.6 nM.

XS-060 is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=1.3 uM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.