RK-701 is a highly selective, potent, and low-toxicity inhibitor of histone methyltransferases G9a and GLP1 with IC50 values of 23-27 nM and 53 nM. RK-701 treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. RK-701 is used in the research of sickle cell disease.