GSK-2879552

Research use only, not for human use.

A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM.

A potent, selective irreversible inhibitor of LSD1 with Ki app of 1.7 uM; shows good selectivity against LSD2, MAO-A, MAO-B, D-amino acid oxidase and LoxL2; exhibits growth inhibition (EC50=2-240 nM) in sensitive cell lines; orally bioavailable.Lung Cancer Phase 1 Clinical.

Cell Proliferation Assay.Cell Line:9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration:0-10000 nM.Incubation Time:6 days.Result:Inhibited cell proliferation.RT-PCR.Cell Line:Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration:0, 1, 2 μM.Incubation Time:24 h.Result:Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

Animal Model:NCI-H526 and NCI-H1417 xenografts.Dosage:1.5 mg/kg.Administration:PO daily for 25-35 days.Result:There was 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 demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

GSK2879552

Chromatin/Epigenetic

Histone Demethylase

LSD1

Cancer

Lung Cancer

1401966-69-5

364.4806

C23H28N2O2

>98% (HPLC)

10 mM in DMSO

O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1

Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years