Chemical Structure : RK-552
CAS No.:
313527-11-6
RK-552
(RK-0080552)
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.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
265.23
|
|
Formula
|
C13H7N5O2
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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
|
References
1. Sae Matsuoka, et al. Blood Neoplasia. 2025 Mar 11;2(2):100091.
Contact Us
sales@probechem.com
