RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 µM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 µM) and SET7/9 (IC50: >50 µM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma[1].
Molecular Weight:
266.22
CAS Number:
[313527-11-6]
Formula:
C12H6N6O2
Target:
Apoptosis,Histone Methyltransferase
Application Notes:
MCE Product type: Reference compound
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