GSK690

Modify Date: 2024-01-06 15:18:58

Use of GSK690

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

Name	4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile
Synonym	More Synonyms

Description	GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Demethylase
In Vitro	GSK690 (1-10μM) 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].
References	[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.

Benzonitrile, 4-[2-(4-methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl]-

4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile

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