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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.
Catalog NO: CT-GSK287
CAS NO: 1401966-69-5, 1401966-63-9
Mol. Formula: C23H28N2O2 ∙ 2HCl
MW: 437.4 (or refer to COA, batch-specific)
** in vivo Quality Material. >99% Pure by Achiral and Chiral HPLCs, Dihydrochloride salt, validated with a high-precision quantitative elemental analysis. Water soluble. Bulk (Pls ask for bulk quote). Prompt.