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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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.
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Choose Selective Histone Demethylase Inhibitors
|Description||GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.|
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. 
|In vivo||In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. |
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.
|In vitro||Water||44 mg/mL (100.59 mM)|
|DMSO||29 mg/mL (66.3 mM)|
* 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.
|CAS No.||1401966-69-5 (free base)|
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02034123||Terminated||Carcinoma Small Cell||GlaxoSmithKline||February 4 2014||Phase 1|
|NCT02929498||Recruiting||Myelodysplastic Syndrome||GlaxoSmithKline|Parexel||July 31 2017||Phase 2|
|NCT02177812||Terminated||Leukaemia Myelocytic Acute||GlaxoSmithKline||August 27 2014||Phase 1|
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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