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Chemical Structure : EZM 2302
CAS No.: 1628830-21-6
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $228 | In stock | |
| 25 mg | $398 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 585.102 | |
| Formula | C29H37ClN6O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
100 mM in DMSO |
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| 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 |
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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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