APS-2-79 hydrochloride NEW
| Price | $39 | $65 | $158 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-04 |
Product Details
| Product Name: APS-2-79 hydrochloride | CAS No.: 2002381-31-7 |
| Purity: 98.64% | Supply Ability: 10g |
| Release date: 2024/11/04 |
Product Introduction
Bioactivity
| 名稱 | APS-2-79 hydrochloride |
| 描述 | APS-2-79 hydrochloride (APS-2-79 HCl) is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. |
| 細胞實驗 | Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the timecourse of assays. Specifically, A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors for 72hrs. Cell viability is measured using resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls(Only for Reference) |
| 激酶實驗 | JNK phosphorylation: 500,000 cells/well are seeded in 6-well plates and incubated overnight. Cells are then incubated for 1 h with test compounds or DMSO as vehicle control (?nal concentration 1% v/v). Puromycin is added (?nal concentration of 18 μM) and cells incubated for a further 10 min to label nascent polypeptide chains. Background labelling is determined by incubating cells without puromycin. Cells are then washed in HBSS, harvested by scraping and centrifuged (300 g, 5 min). Cells are resuspended in 0.5 mL 50 mM DTT containing phosphatase inhibitors and incubated at 95℃ for 10 min. Samples are then snap frozen in liquid nitrogen and stored at -20℃ until blotted. Samples (20–30 μg protein/sample) are blotted onto a PVDF membrane. The membrane is blocked and incubated with anti-phospho-Thr183/Tyr185-JNK antibody overnight at 4℃. Secondary antibodies are used to label the primary antibody and detected using an infrared scanner. The intensity of the ?uorescence signal for anti-phospho-JNK antibody is background corrected and normalized for loading. |
| 體外活性 | APS-2-79 functions as an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site. APS-2-79 is inactive when KSR was absent or when the KSR2(A690F) mutant was used for in vitro assays. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling[1]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 90 mg/mL (212.3 mM) Ethanol : 30 mg/mL (70.8 mM) |
| 關鍵字 | MAP2K | MAPKK | Inhibitor | Mitogen-activated protein kinase kinase | APS 2 79 hydrochloride | APS279 hydrochloride | inhibit | MEK | APS-2-79 Hydrochloride |
| 相關產(chǎn)品 | Vemurafenib | CMPD1 | Lidocaine | SKLB-163 | sodium lauroyl-α-hydroxyethyl sulfonate | Lidocaine hydrochloride | Selumetinib | Takinib | NG25 | Honokiol | Pelitinib | Trametinib |
| 相關庫 | 細胞凋亡化合物庫 | 抗胰腺癌化合物庫 | 經(jīng)典已知活性庫 | 疼痛相關化合物庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 抗肥胖化合物庫 | 抑制劑庫 | 已知活性化合物庫 | MAPK 抑制劑庫 |
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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