GSK2879552

Cas No.:	1401966-69-5
Chemical Name:	GSK2879552,GSK-2879552,GSK 2879552
Synonyms:	GSK2879552,GSK-2879552,GSK 2879552
SMILES:	C1=CC=CC=C1[C@@H]1[C@@H](NCC2CCN(CC3=CC=C(C(O)=O)C=C3)CC2)C1.Cl.Cl
Formula:	C23H28N2O2.2HCl
M.Wt:	437.4
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
In Vivo:	GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice[2].
In Vitro:	GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1]. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min−1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM[2].