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GSK2879552

Catalog No. T3677 CAS 1401966-69-5

Synonyms: GSK2879552 2HCl

GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GSK2879552, CAS 1401966-69-5

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2 mg	In stock	$ 52.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity.
Targets&IC50	LSD1:1.7 μM(Ki)
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. [1]
In vivo	In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1]
Kinase Assay	LSD1 enzyme assay: LSD1 activity was measured using a horseradish peroxidase (HRP) coupled assay with amplex red as an electron donor. The formation of product over time is measured using fluorescence intensity, Ex 531 nm and Em 595 nm, in a PerkinElmer EnVision plate reader. Final assay conditions are: 5 nM LSD1, 2.5 μM H3K4me2 peptide, 50 mM HEPES pH 7, 1 U/ml of HRP, 1 mM CHAPS, 0.03% dBSA and 10 μM amplex red.
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)

Synonyms	GSK2879552 2HCl
Molecular Weight	364.48
Formula	C23H28N2O2
CAS No.	1401966-69-5

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: <1 mg/mL

DMSO: 27 mg/mL(74.1 mM)

References and Literature

1. Mohammad HP, et al. Cancer Cell. 2015, 28(1), 57-69.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK2879552 1401966-69-5 Chromatin/Epigenetic Histone Demethylase inhibit GSK 2879552 GSK2879552 2HCl Inhibitor GSK-2879552 inhibitor

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