LG 100268

LG 100268 is an agonist of retinoid X receptors (RXRs; K_d = 3 nM).¹ It is selective for RXRs over retinoic acid receptors (RARs; K_d = >10,000 nM).² In vitro, LG 100268 (1 µM) induces apoptosis in HL-60 human leukemia cells when used in combination with TTNPB (Item No. 16144).¹ LG 100268 (100, 300, and 1,000 nM) dose-dependently inhibits COX-2 expression and increases ATP-binding cassette transporter (ABCA1) levels in macrophage-like RAW 264.7 cells.³ In vivo, it inhibits vinyl carbamate-induced lung tumor growth in mice when administered at a dose of 40 mg/kg.

WARNING This product is not for human or veterinary use.

1. Boehm, M.F., Zhang, L., Zhi, L., et al. Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells. J. Med. Chem. 38(16), 3146-3155 (1995).

2. Bissonnette, R.P., Brunner, T., Lazarchik, S.B., et al. 9-cis retinoic acid inhibition of activation-induced apoptosis is mediated via regulation of fas ligand and requires retinoic acid receptor and retinoid X receptor activation. Mol. Cell. Biol. 15(10), 5576-5585 (1995).

3. Cao, M., Royce, D.B., Risingsong, R., et al. The rexinoids LG100268 and LG101506 inhibit inflammation and suppress lung carcinogenesis in A/J mice. Cancer Prev. Res. (Phila.) 9(1), 105-114 (2016).