RK-552 | NSD2 inhibitor | Probechem Biochemicals

Chemical Structure : RK-552

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RK-552 (RK-0080552)

货号: 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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	265.23
分子式	C13H7N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(4-methyl-1,2,5-oxadiazol-3-yl)-9H-indeno[1,2-e][1,2,4]triazin-9-one

参考文献

1. Sae Matsuoka, et al. Blood Neoplasia. 2025 Mar 11;2(2):100091.

RK-552 (RK-0080552)

生物&药学活性

物理化学性质&存储条件

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RK-552 (RK-0080552)

生物&药学活性

物理化学性质&存储条件

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