GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

GSK-2879552,GSK 2879552

Powder

Water 44 mg/mL (100.59 mM)

DMSO 29 mg/mL (66.3 mM)

Histone Demethylase

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. 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.

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.