GNF-2 NEW
| Price | $37 | $59 | $122 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: GNF-2 | CAS No.: 778270-11-4 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | GNF-2 |
| 描述 | GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl. |
| 細胞實驗 | Cells (0.3-0.6 × 106 per mL) are plated in duplicate or triplicate in 96-well plates containing increasing GNF-2 concentrations (5 nM–10 μM). After incubation at 37 ℃ in 5% CO2 for 48 hours, the effect of GNF-2 on cell viability is determined by the MTT colorimetric dye reduction method. Inhibition of cell proliferation is calculated as a percentage of growth of DMSO-treated cells, and IC50 values are determined with Microsoft Excel XLfit3.(Only for Reference) |
| 激酶實驗 | Binding assay: Recombinant proteins (100 nM for each construct) or immunoprecipitated proteins are diluted in kinase buffer (20 mM HEPES (pH 7.4), 50 mM KCl, 0.1% CHAPS, 30 mM MgCl2, 2 mM MnCl2, 1 mM DTT, and 1% glycerol). Aliquots of the diluted proteins are preincubated with either DMSO or compounds for 30 min at room temperature and then added to K-LISA PTK EAY reaction plates. The kinase reaction is initiated by adding 0.1 mM ATP and is allowed to proceed for 30 min at room temperature. The phosphorylation of GST-Abltide is monitored by SDS-PAGE and phosphorimaging analysis or autoradiography. |
| 體內(nèi)活性 | GNF-2, at a concentration of 1 μM, induces apoptosis in Ba/F3.p210 and Ba/F3.p210E255V cells and significantly reduces phosphorylated Stat5 levels in Ba/F3.p210 cells. It inhibits Bcr-abl tyrosine phosphorylation in a dose-dependent manner, with an IC50 value of 267 nM. Furthermore, 10 μM GNF-2 inhibits BCR-Abl-dependent cell proliferation, requiring the BCR and/or c-Abl SH3 and/or SH2 domains, and significantly suppresses CrkII tyrosine phosphorylation in a dose-dependent manner. GNF-2 demonstrates an inhibition effect on CrkII phosphorylation in cells expressing c-AblG2A, with an IC50 of 0.051 μM, and inhibits autophosphorylation and proliferation in cells expressing p210Bcr-Abl and its mutants, BafF3. When combined with GNF-5 (20 nM), GNF-2 (8 nM) shows a synergistic effect in inhibiting Abl64-515 kinase activity. It also exhibits dose-dependent inhibitory effects on the growth of Bcr-abl positive cells (IC50 values: 273 nM for K562 and 268 nM for SUP-B15) and Ba/F3.p210E255V and Ba/F3.p185Y253H cells, with IC50 values of 268 nM and 194 nM, respectively. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 37.4 mg/mL (100 mM) Ethanol : 18.7 mg/mL (50 mM) |
| 關(guān)鍵字 | SARS coronavirus | allosteric | non-ATP competitive inhibitor | Ba/F3.p185Y253H | Bcr-Abl | Ba/F3.p210E255V | GNF-2 | SARS-CoV | Ba/F3.p210 | bone erosion | Inhibitor | GNF 2 | inhibit |
| 相關(guān)產(chǎn)品 | Nirmatrelvir | EIDD-1931 | Remdesivir | Andrographolide | Silymarin | Umifenovir hydrochloride | Hydroxychloroquine | Ritonavir | Chloroquine phosphate | Chloroquine | Favipiravir | Imatinib |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 酪氨酸激酶分子庫 | 抗病毒庫 | 血管生成庫 | 抑制劑庫 | 已知活性化合物庫 | 含氟化合物庫 | 細胞骨架化合物庫 |
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
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