GSK3368715 (EPZ019997) 3HCl |
| カタログ番号GC25483 |
GSK3368715は、PRMT1、3、4、6および8を抑制するタイプIタンパク質アルギニンメチルトランスフェラーゼ（PRMT）の強力な阻害剤であり、Kiapp値は1.5〜81 nMの範囲である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2227587-26-8
Sample solution is provided at 25 µL, 10mM.
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GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.[1]
GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.[1]
[1] Andrew Fedoriw, et al. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.
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