I-BET151 NEW
| Price | $41 | $59 | $97 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: I-BET151 | CAS No.: 1300031-49-5 |
| Purity: 99.63% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | I-BET151 |
| 描述 | I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays). |
| 細(xì)胞實(shí)驗(yàn) | Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader (Only for Reference) |
| 激酶實(shí)驗(yàn) | Fluorescence anisotropy (FP) ligand displacement assay: All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM). |
| 體外活性 | I-BET151 administration (30 mg/kg/day) in mice significantly inhibits the growth of MLL-AF9 murine and MLL-AF4 human leukemia tumors and notably prolongs lifespan. |
| 體內(nèi)活性 | When interacting with HL60 nuclear extracts, I-BET151 at concentrations of 0.5 or 5 μM inhibits the binding of BETs (BRD2/3/4/9) to acetylated histone peptides without affecting 23 other bromodomain proteins. This compound demonstrates potent inhibitory effects on cell lines with various MLL fusions, such as MV4;11, RS4;11, MOLM13, and NOMO1 cells (IC50: 15-192 nM). I-BET151 shows broad selectivity in inhibiting multiple protein types, including COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 possesses a high binding affinity for BRD2/3/4 (Kd: 0.02-0.1 μM) and significantly inhibits the production of the IL-6 cytokine in response to lipopolysaccharide stimulation in human peripheral blood mononuclear cells, whole blood, and rat WB (IC50: 0.16/1.26/1.26 μM). |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (120.35 mM) |
| 關(guān)鍵字 | I-BET-151 | I BET151 | inhibit | bromodomain | BET | Epigenetic Reader Domain | BRD2 | Inhibitor | BRD4 | I-BET 151 | BRD3 | I-BET151 | IBET151 |
| 相關(guān)產(chǎn)品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
| 相關(guān)庫(kù) | 組蛋白修飾化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 染色質(zhì)修飾分子庫(kù) | 抑制劑庫(kù) | 干細(xì)胞分化化合物庫(kù) | NO PAINS 化合物庫(kù) | PPI抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) |
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.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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