Home Epigenetics Histamine Receptor inhibitor - Histone Demethylase inhibitor - LSD1 inhibitor GSK2879552 2HCl For research use only.

GSK2879552 2HCl

GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.

GSK2879552 2HCl Chemical Structure

GSK2879552 2HCl Chemical Structure

CAS No. 1902123-72-1

Purity & Quality Control

GSK2879552 2HCl Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 Function assay 0, 7, 47, and 3000 nM 1 day a dose-dependent increase in CD11b and CD86 expression with average EC50 values of 23 +/- 4 nM 30514804
MOLM-13 Proliferation assay 6 days dose responsive decrease in BrdU signal, EC50 = 1.9 +/- 0.9 nM 30514804
MV4-11 Antiproliferative assay 240 hrs Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay, IC50=1.16μM 30713023
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Biological Activity

Description GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
Targets
LSD1 [1]
(Cell-free assay)
1.7 μM(Ki)
In vitro
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]
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 Cell lines 165 human cancer cell lines
Concentrations ~10 μM
Incubation Time 6 d
Method 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot H3 / H3K4me1 / H3K4me2 / LSD1 26175415
Growth inhibition assay Cell viability 30514804
In Vivo
In vivo In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02929498 Terminated
Myelodysplastic Syndrome|Myelodysplastic Syndromes
GlaxoSmithKline|Parexel
 July 31 2017 Phase 1|Phase 2
NCT02177812 Terminated
Leukaemia Myelocytic Acute
GlaxoSmithKline
 August 27 2014 Phase 1
NCT02034123 Terminated
Carcinoma Small Cell
GlaxoSmithKline
 February 4 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 437.4 Formula

C23H28N2O2.2HCl
CAS No. 1902123-72-1 SDF Download GSK2879552 2HCl SDF
Smiles C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 44 mg/mL

DMSO : 29 mg/mL ( (66.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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