For research use only. Not for therapeutic Use.
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].
GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1].
GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice[2].
| Catalog Number | I015338 |
| CAS Number | 1902123-72-1 |
| Synonyms | 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]piperidin-1-yl]methyl]benzoic acid;dihydrochloride |
| Molecular Formula | C23H30Cl2N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H28N2O2.2ClH/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19;;/h1-9,17,21-22,24H,10-16H2,(H,26,27);2*1H/t21-,22+;;/m0../s1 |
| InChIKey | QEKGSBZKRLHQSZ-VSIGASKDSA-N |
| SMILES | C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O.Cl.Cl |
| Reference | [1]. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21. [2]. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69. |
