GSK2879552 NEW
| Price | $109 |
| Package | 2mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: GSK2879552 | CAS No.: 1401966-69-5 |
| Purity: 99.22% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | GSK2879552 |
| Description | GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity. |
| Cell Research | 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.(Only for Reference) |
| Kinase Assay | 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 | 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] |
| In vivo | In SCLC xenograft bearing mice, GSK2879552 (1.5 mg/kg, p.o.) demonstrates tumor growth inhibition by 17%-83%. [1] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : <1 mg/mL DMSO : 27 mg/mL (74.1 mM) |
| Keywords | Inhibitor | inhibit | Histone Demethylase | GSK-2879552 | GSK2879552 | GSK 2879552 |
| Inhibitors Related | LSD1-IN-24 | Tranylcypromine hemisulfate | DDP-38003 dihydrochloride | GSK-LSD1 dihydrochloride | GSK-J4 | FY-21 | Daminozide | Zavondemstat | AS8351 | Procaine hydrochloride | JIB-04 | KDM4-IN-4 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $54.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 | |
| $9.80/1KG |
VIP6Y
|
Career Henan Chemical Co
|
2020-01-09 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY