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GSK2879552 Dihydrochloride LSD1 Inhibitor

Name: GSK2879552 Dihydrochloride
Brand: Selleck Chemicals
SKU: S7796
Availability: InStock
Rating: 5 (29 reviews)

Cat.No.S7796

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

Chemical Structure

Molecular Weight: 437.4

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	Epigenetic Reader Domain HDAC JAK Histone Methyltransferase AMPK PKC PARP HIF Histone Acetyltransferase Aurora Kinase Sirtuin PRMT Histone Demethylase EZH1/2 DNA Methyltransferase Pim LSD1 MLL JMJD G9a/GLP NSD FTO MicroRNA PAD SETD SMYD DOT1 COMT WDR5 HNMT
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	437.4	Formula	C₂₃H₂₈N₂O₂.2HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1902123-72-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O.Cl.Cl

Solubility

In vitro
Batch:

Water : 44 mg/mL

DMSO : 29 mg/mL (66.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.350mg/ml (9.95mM)	Taking the 1 mL working solution as an example, add 50 μL 87 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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]
Kinase Assay	LSD1 enzyme assay
Kinase 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 vivo	In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. ^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/26175415/

Applications

Methods	Biomarkers	Images	PMID
Western blot	H3 / H3K4me1 / H3K4me2 / LSD1		26175415
Growth inhibition assay	Cell viability		30514804

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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