GSK2879552, LSD1 Inhibitor
Overview | |
Catalog # | bs-60297c-2-mg-solid |
Product Name | GSK2879552, LSD1 Inhibitor |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 437.4 Formula: C23 H30 Cl2 N2 O2 CAS Number: 1902123-72-1 InChi Key: QEKGSBZKRLHQSZ-VSIGASKDSA-N InChi: InChI=1S/C23H28N2O2.2ClH/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19;;/h1-9,17,21-22,24H,10-16H2,(H,26,27);2*1H/t21-,22+;;/m0../s1 Smiles: Cl.Cl.OC(=O)C1=CC=C(CN2CCC(CN[C@@H]3C[C@H]3C3C=CC=CC=3)CC2)C=C1 Purity: 98.0 Solubility: DMSO up to 50 mM; Water up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | GSK2879552 is a highly potent, selective and orally bioavailable irreversible inhibitor of Lysine Specific Demethylase 1 (LSD1). It is highly selective over related enzymes such as MAO-A/B. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) is sensitive to GSK2879552’s inhibition. It increases H3K4 methylation selectively at genomic regions bound by LSD1. It demonstrates efficacy in preclinical models of SCLC. Currently GSK2879552 is in phase I clinical trials targeting Acute Myeloid Leukemia (AML) and Relapsed/Refractory Small Cell Lung Carcinoma. |