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EZM 2302

Chemical Structure : EZM 2302

CAS No.: 1628830-21-6

EZM 2302 (GSK 3359088;GSK3359088;EZM2302)

Catalog No.: PC-61030Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: 99.5% (HPLC) Select Batch:

Biological Activity

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.
EZM 2302 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).
EZM 2302 displays dose-dependent inhibition of CARM1 substrate methylation in vivo, and induces growth inhibition of human multiple myeloma tumor xenografts in mice.

Physicochemical Properties

M.Wt 585.102
Formula C29H37ClN6O5
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

100 mM in DMSO

Chemical Name/SMILES

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

References

1. Drew AE, et al. Sci Rep. 2017 Dec 21;7(1):17993.

2. Greenblatt SM, et al. Cancer Cell. 2018 Jun 11;33(6):1111-1127.e5.

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