GSK690(Hydrochloride)是赖氨酸特异性去甲基化酶1(LSD1)的可逆抑制剂，Kd值为9nM，IC50值为37nM。
货号:ajcx13360
CAS:N/A
分子式:C24H24ClN3O
分子量：405.92
溶解度:DMSO : 125 mg/mL (307.94 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.

GSK690 (1-10 μM) acts together with JNJ-26481585 to induce cell death in all four tested RMS cells lines (RD, RH30, RMS13, and TE381.T cells)[2].GSK690/JNJ-26481585 cotreatment alters the balance between pro- and antiapoptotic proteins with 1 μM GSK690 for RD cells and 10 μM GSK690 for RH30 cells[2].GSK690/JNJ-26481585 cotreatment induces caspase-dependent cell death with 1 μM GSK690 for RD cells and 10 μM GSK690 for RH30 cells[2].The addition of GSK690 further enhances the JNJ-26481585-stimulated G2/M arrest [2].

[1]. Mould DP, et al. Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1. J Med Chem. 2017 Oct 12;60(19):7984-7999. [2]. Haydn T, et al. Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis in rhabdomyosarcoma cells. Cell Death Dis. 2017 Jun 15;8(6):e2879.