AM80

AM80 is a retinoic acid receptor agonist that is selective for RARα (K_d = 62 nM; AC₅₀ = 1.46 nM) compared to RARβ (K_d = 280 nM; AC₅₀ = 6.87 nM) and RARγ (K_d = 816 nM; AC₅₀ = 148.7 nM).¹ It demonstrates greater specific binding to RARα compared to retinoic acid (Item No. 11017), which exhibits little selectivity across RARα, β, or γ.^2,1 AM80 exhibits antiproliferative effects against acute promyelocytic leukemia cells, inducing human promyelocytic leukemia HL-60 cell differentiation with an ED₅₀ value of 0.79 nM.^3,2 It has also been shown to suppress the growth of other myeloid and lymphoid malignant cells.²

WARNING This product is not for human or veterinary use.

1. Bernard, B.A., Bernardon, J.-M., Delescluse, C., et al. Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor γ. Biochem. Biophys. Res. Commun. 186(2), 977-983 (1992).

2. Jimi, S., Mashima, K., Matsumoto, T., et al. RARα is a regulatory factor for Am-80-induced cell growth inhibition of hematologic malignant cells. Int. J. Oncol. 31(2), 397-404 (2007).

3. Eyrolles, L., Kagechika, H., Kawachi, E., et al. Retinobenzoic Acids. 6. Retinoid antagonists with a heterocyclic ring. J. Med. Chem. 37, 1508-1517 (1994).