NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC 50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest.