EZM 2302
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.
Product Specifications
CAS Number
1628830-21-6
Product Name Alternative
GSK 3359088 | GSK3359088 | EZM2302
Purity
>98% (HPLC)
Solubility
100 mM in DMSO
Smiles
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
Molecular Formula
C29H37ClN6O5
Molecular Weight
585.102
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
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