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Background Information:
GSK2879552 is an orally bioavailable, potent, selective, and mechanism-based irreversible inhibitor of Lysine specific demethylase 1 (LSD1). LSDI, a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes, including Histone Deacetylases (HDAC1/2) and Co-Repressor for Element-1-Silencing Transcription factor (CoREST). Studies have implicated that LSD1 is a key regulator of the epigenome that modulates gene expression through post-translational modification of histones and through its presence in transcriptional complexes, and is overexpressed in certain tumor cells. Inhibition of LSD1 enhances H3K4 methylation and increases the expression of tumor-suppressor genes. GSK2879552, as a first-in-class LSD1 inhibitor with excellent potency and pharmacological properties, is currently under clinical evaluation for cancer treatment.
APIM050330: GSK2879552
CAS No.: 1401966-69-5, 1401966-63-9.
Molecular Formula: C23H28N2O2 ? 2HCl.
Molecular Weight: 437.4 (or refer to COA, batch-specific).
Purity: 99.9% chemical purity, 100% optical purity, Lot 02.
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO, in Water.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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