Free shipping on all orders over $ 500

GSK126

Cat. No. M2114
GSK126 Structure
Synonym:

EZH2 inhibitor; GSK2816126A

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 40  USD40 In stock
5mg USD 70  USD70 In stock
10mg USD 108  USD108 In stock
50mg USD 286  USD286 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 2. GSK126
Method Clonogenicity
Cell Lines multiple myeloma cells
Concentrations 10 μM
Incubation Time 24 h
Results The results showed that after exposure to GSK126 for 24 h, the colonyformation ability of MM cells were significantly reduced with IC50 < 10 μM
Protocol (for reference only)
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
Chemical Information
Molecular Weight 526.67
Formula C31H38N6O2
CAS Number 1346574-57-9
Solubility (25°C) DMSO 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Sato T, et al. Sci Rep. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer.

[2] McCabe MT, et al. Nature. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.

Related EZH2 Products
Tulmimetostat

Tulmimetostat is an orally active dual EZH1/EZH2 protein inhibitor with antitumor activity for use in a variety of solid tumor studies.

PF-06821497

PF-06821497 is a selective and orally active Zeste Homolog 2 (EZH2) inhibitor with powerful tumor growth inhibition.

CPI-1205

CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.

Valemetostat

Valemetostat (DS-3201, DS-3201b) is a first-in-class dual inhibitor targeting EZH1 and EZH2. It can be used in the study of adult T-cell leukemia/lymphoma.

MS1943

MS1943 is a pioneering oral bioactive selective EZH2 inhibitor with an IC50 of 120 nM. MS1943 significantly reduced EZH2 protein levels in many triple negative breast and other cancers and non-cancer lines. MS1943 effectively blocked the proliferation of multiple triple negative breast cancers and other cancer lines.

  Catalog
Abmole Inhibitor Catalog




Keywords: GSK126, EZH2 inhibitor; GSK2816126A supplier, EZH2, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.