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GSK126

Cat. No. M2114
GSK126 Structure
Size Price Availability Quantity
10mg USD 115 In stock
50mg USD 290 In stock
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Quality Control
Biological Activity

GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.

Protocol
Cell Experiment
Cell lines EZH2 wildtype or mutant B-cell lymphoma cell lines
Preparation method Cell proliferation assay. The optimal cell seeding was 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 were then plated at the optimal seeding density 24 h before treatment (in duplicate) with a 20-point twofold dilution series of GSK126 or 0.15% DMSO. Plates were incubated for 6 days at 37℃ in 5% CO2. Cells were then lysed with CellTiter-Glo (CTG) (Promega) and chemiluminescent signal was detected with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells was harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values obtained after the 6 day treatment were expressed as a percent of the T0 value and plotted against compound concentration. Data were 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) was determined.
Concentrations 0~100µM
Incubation time 6 days
Animal Experiment
Animal models Pfeiffer or KARPAS-422 cells tumour xenograft in mice
Formulation 20% captisol adjusted to pH 4–4.5 with 1 N acetic acid.
Dosages 0.2 ml per 20 g body weight
Administration intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 526.67
Formula C31H38N6O2
CAS Number 1346574-57-9
Purity 99.26%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer.
Sato T, et al. Sci Rep. 2013;3:1911. PMID: 23714854.

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe MT, et al. Nature. 2012 Dec 6;492(7427):108-12. PMID: 23051747.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK126 supplier, EZH2, inhibitors

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