EZM 2302

Research use only, not for human use.

EZM 2302 (EZM2302, GSK 3359088)is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM.

EZM 2302 (EZM2302, GSK 3359088)is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM, with broad selectivity against other HMTases; demonstrates in vitro anti-proliferative activity consistent with specific methyl mark inhibition with IC50 of <100 nM in 9/15 multiple myeloma cell lines, decreases methylation of PABP1 (IC50=38 nM) and SmB (IC50=18 nM); displays dose-dependent inhibition of CARM1 substrate methylation in vivo, and induces growth inhibition of human multiple myeloma tumor xenografts in mice.

GSK 3359088;GSK3359088;EZM2302

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

1628830-21-6

585.10

C29H37ClN6O5

99.5% (HPLC)

100 mM in DMSO

O=C(N(CC1)CCC21CN(C3=NC(C4=CC(OC[C@H](O)CNC)=CC=C4Cl)=NC(C5=C(C)ON=C5C)=C3C)C2)OC

methyl (R)-2-(2-(2-chloro-5-(2-hydroxy-3-(methylamino)propoxy)phenyl)-6-(3,5-dimethylisoxazol-4-yl)-5-methylpyrimidin-4-yl)-2,7-diazaspiro[3.5]nonane-7-carboxylate

(-20℃)

With Ice Pack

≥ 2 years