價(jià)格 | ¥793 | ¥389 |
包裝 | 5mg | 2mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 GSK2879552 | 英文名稱:GSK2879552 |
CAS:1401966-69-5 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.22% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T3677 |
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 | 在165個(gè)細(xì)胞系中,GSK2879552對(duì)9/28個(gè)小細(xì)胞肺癌(SCLC)系和20/29個(gè)AML系的生長抑制率在40%至100%之間。對(duì)于對(duì)GSK2879552產(chǎn)生生長抑制反應(yīng)的SCLC細(xì)胞系和初級(jí)樣本子集,顯示出一組特征探針的DNA低甲基化。[1] |
In vivo | 在攜帶SCLC異種移植瘤的小鼠中,GSK2879552(1.5 mg/kg,p.o.)展現(xiàn)了17%-83%的腫瘤生長抑制效果。[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 | DDP-38003 dihydrochloride | Zavondemstat | FY-21 | KDM4-IN-4 | Procaine hydrochloride | JIB-04 | GSK-J4 | LSD1-IN-24 | Daminozide | AS8351 | GSK-LSD1 dihydrochloride | Tranylcypromine hemisulfate |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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