For research use only. Not for therapeutic Use.
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].
| Catalog Number | I046260 |
| CAS Number | 2436760-79-9 |
| Synonyms | 4-[2-(4-methylphenyl)-5-[[(3R)-pyrrolidin-3-yl]methoxy]pyridin-3-yl]benzonitrile;hydrochloride |
| Molecular Formula | C24H24ClN3O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H23N3O.ClH/c1-17-2-6-21(7-3-17)24-23(20-8-4-18(13-25)5-9-20)12-22(15-27-24)28-16-19-10-11-26-14-19;/h2-9,12,15,19,26H,10-11,14,16H2,1H3;1H/t19-;/m1./s1 |
| InChIKey | DBTSJYXXWZFXNJ-FSRHSHDFSA-N |
| SMILES | CC1=CC=C(C=C1)C2=C(C=C(C=N2)OCC3CCNC3)C4=CC=C(C=C4)C#N.Cl |
| Reference | [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. |
