GSK2879552 2HCl

Catalog No.S7796

For research use only.

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

GSK2879552 2HCl Chemical Structure

CAS No. 1902123-72-1

Selleck's GSK2879552 2HCl has been cited by 18 publications

Purity & Quality Control

Choose Selective Histamine Receptor Inhibitors

Other Histamine Receptor Products

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 NHf1TZZHfW6ldHnvckBie3OjeR?= MlTkNEwhPyxiNEesJIFv\CB|MECwJI5O M36yc|Eh\GG7 MX7hJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGNFOTGkIHHu[EBETDh4IHX4dJJme3Orb36ge4l1cCCjdnXyZYdmKEWFNUCgeoFtfWW|IH;mJFI{KCtxLTC0JI5O MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODVzNEiwOEc,OzB3MUS4NFQ9N2F-
MOLM-13 NI\aUI1Rem:uaX\ldoF1cW:wIHHzd4F6 M{TQUlYh\GG7cx?= NVH6[5py\G:|ZTDy[ZNxd26|aY\lJIRm[3KnYYPlJIlvKEK{ZGWgd4lodmGuLDDFR|UxKD1iMT65JEswNSByLkmgcm0> MlvuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3MUS4NFQoRjNyNUG0PFA1RC:jPh?=
MV4-11 NFi4RZNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mmj2NlQxKGi{cx?= MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB{NECgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1zLkG2{txO NEfOXpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEexN|AzOyd-M{C3NVMxOjN:L3G+
Assay
Methods Test Index PMID
Western blot H3 / H3K4me1 / H3K4me2 / LSD1 26175415
Growth inhibition assay Cell viability 30514804
In vivo In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 437.4
Formula

C23H28N2O2.2HCl

CAS No. 1902123-72-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02929498 Terminated Drug: GSK2879552|Drug: Azacitidine Myelodysplastic Syndrome|Myelodysplastic Syndromes GlaxoSmithKline|Parexel July 31 2017 Phase 1|Phase 2
NCT02177812 Terminated Drug: GSK2879552|Drug: ATRA Leukaemia Myelocytic Acute GlaxoSmithKline August 27 2014 Phase 1
NCT02034123 Terminated Drug: GSK2879552 Carcinoma Small Cell GlaxoSmithKline February 4 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy GSK2879552 2HCl | GSK2879552 2HCl supplier | purchase GSK2879552 2HCl | GSK2879552 2HCl cost | GSK2879552 2HCl manufacturer | order GSK2879552 2HCl | GSK2879552 2HCl distributor