GSK690

Names

[ Name ]:
GSK690

[Synonym ]:
Benzonitrile, 4-[2-(4-methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl]-
4-{2-(4-Methylphenyl)-5-[(3R)-3-pyrrolidinylmethoxy]-3-pyridinyl}benzonitrile

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
530.5±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₃N₃O

[ Molecular Weight ]:
369.459

[ Flash Point ]:
274.6±30.1 °C

[ Exact Mass ]:
369.184113

[ LogP ]:
3.75

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.640

Related Compounds

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