(±)-MRJF22, a prodrug of the sigma (σ) ligand haloperidol metaboliteII conjugated with the histone deacetylase (HDAC) inhibitor valproicacid, has previously demonstrated a promising antiangiogenic activity.Herein, the asymmetric synthesis of (R)-(+)-MRJF22 and (S)-(−)-MRJF22 was performed to investigate their contributionto (±)-MRJF22 antiangiogenic effects in human retinalendothelial cells (HREC) and to assess their therapeutic potentialin primary human uveal melanoma (UM) 92-1 cell line. This evidence concerns the gene HDAC9 and uveal melanoma.