AM580

AM580 is a retinoic acid receptor (RAR) agonist that is selective for RARα (EC₅₀ = 0.36 nM) compared to RARβ (EC₅₀ = 24.6 nM) and RARγ (EC₅₀ = 27.9 nM; Bernard et al.) It is a derivative of retinoic acid (RA), however it demonstrates greater specific binding to RARα compared to RA, which exhibits little selectivity across RARα, β, or γ (Gianní et al.; Bernard et al.; Kim et al; Rochette-Egly & Germain).

REPROGRAMMING

• Promotes reprogramming of somatic cells to induced pluripotent stem cells (Wang et al.).

DIFFERENTIATION

• Induces differentiation of human induced pluripotent stem cells into intermediate mesoderm, in combination with the GSK3β inhibitor CHIR99021 (Araoka et al.).

CANCER RESEARCH

• Inhibits tumor cell proliferation and survival signaling pathways, and induces apoptosis, leading to inhibition of mouse mammary tumor virus (MMTV)-neu- and MMTV-wnt1-induced mammary gland hyperplasia (Lu et al.).
• Inhibits tumor growth in MMTV-Myc mice (Bosch et al.).
• Inhibits endometrial cancer cell proliferation (Cheng et al.).
• Induces differentiation in acute promyelocytic leukemia cells (Gianní et al.).