LG-100268

LG‑100268 is a potent, selective, and orally active small molecule agonist of the retinoid X receptor (RXR) family. It was developed by Ligand Pharmaceuticals as an experimental rexinoid for research purposes. The compound displays high selectivity for RXRs over retinoic acid receptors (RARs), with EC50 values in the low nanomolar range for RXRα, RXRβ, and RXRγ. Mechanistically, it activates both RXR homodimers and heterodimers (notably with PPARγ), leading to transcriptional activation of target genes involved in metabolism, cell differentiation, and proliferation. Preclinical studies have demonstrated efficacy in models of obesity, diabetes (improving glycemic control), breast cancer prevention (especially when combined with tamoxifen), lung cancer prevention/treatment models, and modulation of thyroid axis hormones. Notably, it induces tissue transglutaminase activity in leukemia cells and has pronounced effects on liver metabolism including hepatomegaly[1][2][3][4][5][6][7][8].

Other names

lg100268lg-100268lg 100268LGD 100268LGD100268LGD-100268