GSK2879552 2HCl

For research use only.

Catalog No.S7796

7 publications

GSK2879552 2HCl Chemical Structure

Molecular Weight(MW): 437.4

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

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Selleck's GSK2879552 2HCl has been cited by 7 publications

1 Customer Review

  • Effects of LSD1 inhibitors in acute myeloid leukaemia cells. Cells were exposed to drugs for 48 h or for the indicated times. Cell death and Dwm dissipation were determined by flow cytometric analyses of propidium iodide uptake or DiOC6(3) staining, respectively. Caspase 3/7 activity was determined using the fluorogenic substrate Ac-DEVD-AMC; relative caspase 3/7 activities are the ratio of treated cells to untreated cells. Means±SEM of each two (caspase 3/7 activity) or three (flow cytometric analyses) separate measurements are shown.

    Br J Haematol, 2017, doi: 10.1111/bjh.14983. GSK2879552 2HCl purchased from Selleck.

Purity & Quality Control

Choose Selective LSD1 Inhibitors

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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
THP-1 NGnlWZZHfW6ldHnvckBie3OjeR?= Mn3mNEwhPyxiNEesJIFv\CB|MECwJI5O NWTabm41OSCmYYm= MVPhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGNFOTGkIHHu[EBETDh4IHX4dJJme3Orb36ge4l1cCCjdnXyZYdmKEWFNUCgeoFtfWW|IH;mJFI{KCtxLTC0JI5O NGPWc2Q{ODVzNEiwOC=>
MOLM-13 NX30cXpGWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3fve|Yh\GG7cx?= Mm\Y[I9{\SC{ZYPwc45{cX[nIHTlZ5Jm[XOnIHnuJGJz\FVic3nncoFtNCCHQ{WwJF0hOS57IDuvMUAxNjlibl2= NV;Ld|l7OzB3MUS4NFQ>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
H3 / H3K4me1 / H3K4me2 / LSD1 ; 

PubMed: 26175415     


Western analysis of global H3K4me1 and H3K4me2 from NCI-H526 cell lysates after 24 hr of treatment with GSK2879552. The recombinant histones with specific modifications were used as antibody controls. Histone H3 and tubulin were used as the loading controls.

26175415
Growth inhibition assay
Cell viability; 

PubMed: 30514804     


Dose response curves of MOLM-13 (left) and OCI-AML3 (right) cells treated with a titration of GSK2879552 ± 1, 10, 100, or 1000 nM ATRA for four days. Values were graphed relative to the appropriate ATRA alone concentration for each curve.

30514804
In vivo In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1]

Protocol

Kinase Assay:[1]
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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:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro Water 44 mg/mL (100.59 mM)
DMSO 29 mg/mL (66.3 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 437.4
Formula

C23H28N2O2.2HCl

CAS No. 1902123-72-1
Storage powder
in solvent
Synonyms N/A
Smiles Cl.Cl.OC(=O)C1=CC=C(CN2CCC(CC2)CNC3CC3C4=CC=CC=C4)C=C1

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID