Catalog No.: PC-25565Not For Human Use, Lab Use Only.
RK-0080552 (RK-552) is a potent, specific small molecule NSD2 inhibitor with IC50 of 0.11 uM, weakly inhibits G9a (IC50=1.2 uM) and does not inhibit SET7/9.
RK-0080552 (RK-552) is a potent, specific small molecule NSD2 inhibitor with IC50 of 0.11 uM, weakly inhibits G9a (IC50=1.2 uM) and does not inhibit SET7/9.
RK-552 is cytotoxic to t(4;14)+ MM cells in vitro via NSD2 inhibition at 0-4 uM range.
RK-552 influenced gene expression in favor of cell death in MM cells carrying t(4;14).
RK-552 reduced the expression of major MM growth and survival factors, such as HIF1A, IRF4, MYC, SLAMF7, and CCND2 in t(4;14)+ MM cells, induced downregulation of IRF4 protein and mRNA.
RK-552 decreased H3K36me2 at the whole-genome level.
RK-552 (10 mg/kg, i.p.) inhibited tumor growth of t(4;14)+ MM cells in vivo.
