GSK2879552

SKU: orb1693457

Description

GSK2879552 is an orally active, irreversible, and selective mechanism-based inhibitor of lysine-specific demethylase 1 (LSD1). It exhibits antineoplastic activity and has been investigated in preclinical studies, including in vitro assays and in vivo models, for cancers such as small cell lung carcinoma and acute myeloid leukemia.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1401966-69-5
• MW: 364.48
• Purity: 99.22%
• Formula: C₂₃H₂₈N₂O₂
• SMILES: OC(=O)c1ccc(CN2CCC(CN[C@@H]3C[C@H]3c3ccccc3)CC2)cc1
• Target: Histone Demethylase
• Solubility: DMSO:27 mg/mL (74.08 mM);Ethanol:<1 mg/mL;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.49 mM)

Bioactivity

• Target IC50:
  LSD1:1.7 μM(Ki)
• In Vivo:
  In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%.
• In Vitro:
  In 165 cell lines, GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines ranged from 40% to 100%. The subset of SCLC lines and primary samples that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes.
• Cell Research:
  The optimal cell seeding is determined empirically for all cell lines by examining the growth of a wide range of seeding densities in a 384-well format to identify conditions that permitted proliferation for 6 days. Cells are then plated at the optimal seeding density 24 h before treatment (in duplicate) with a 20-point twofold dilution series of GSK2879552 or 0.15% DMSO. Plates are incubated for 6 days at 37°C in 5% CO2. Cells are then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal is detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6 day treatment are expressed as a percent of the T0 value and plotted against compound concentration. Data are fit with a four-parameter equation to generate a concentration response curve and the concentration of GSK126 required to inhibit 50% of growth (growth IC50) is determined.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LSD1, GSK 2879552, GSK 2879552 HCl, GSK2879552, GSK-2879552, GSK2879552 2HCl, GSK2879552 2HCl, HistoneDemethylase, Histone Demethylase

Compound Identifiers

PubChem CID

66571643