YM-58483 NEW
| Price | $30 | $43 | $68 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: YM-58483 | CAS No.: 223499-30-7 |
| Purity: 99.93% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | YM-58483 |
| 描述 | YM-58483 (BTP2) is a specific and effective inhibitor of CRAC channels and subsequent Ca2+ signals. |
| 細(xì)胞實驗 | Jurkat cells (1×107 cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb. (Only for Reference) |
| 激酶實驗 | HCT-116 cells are washed with PBS and then homogenized with a 27-gauge syringe in binding buffer (10 mm Tris-HCl (pH 7.4), 50 mm KCl, 5 mm MgCl2, 1 mm EDTA, and 0.1 mm Na3VO4). The cell lysate is centrifuged at 13,000 rpm for 30 min at 4°C, and the supernatant is collected. The HCT-116 cell lysate supernatant is precleared by incubating with Dynabeads M-280 streptavidin for 30 min at 4°C and captured by magnet separation. The cleared supernatants are incubated with biotinyl-KRIBB11 compound. After overnight incubation at 4°C, proteins associated with the biotinyl-KRIBB11 compound are precipitated with Dynabeads M-280 streptavidin. Precipitated samples are separated by a magnet. Samples are washed with 1 mL of ishing buffer containing 50 mm HEPES (pH 7.5), 50 mm NaCl, 1 mm EDTA, 1 mm EGTA, 0.1% Tween 20, 10% (v/v) glycerol, 1 mm NaF, 0.1 mm Na3VO4, and protease inhibitor mixture tablets (1 tablet/10 mL). Samples are boiled in SDS-PAGE sample buffer, separated by 10% polyacrylamide gel, and immunoblotted with antibodies against HSF1, HSF2, HSP90, or CDK9. |
| 體外活性 | In various models of allergic asthma, including airway hyperresponsiveness, early and late-phase bronchoconstriction, and antigen-induced airway eosinophilia, YM-58483 demonstrates inhibitory effects. Furthermore, in rat and guinea pig tissues, it reduces levels of leukotrienes and IL-4. In mice with GVHD, YM-58483 also suppresses host-versus-graft CTL reactions, donor T cell proliferation, and the production of IFN-γ. Notably, YM-58483 (30 mg/kg, p.o.) does not significantly affect general activity in mice [1]. |
| 體內(nèi)活性 | As a selective SOCE inhibitor, YM-58483 inhibits sustained calcium ion influx induced by anti-CD3 antibodies in Jurkat T cells. It inhibits CRAC, TRPC3, and TRPC5 channels, while promoting the TRPM4 channel, leading to the suppression of cytokine production (IL-2, IL-4, IL-5, IFN-γ, etc.) and T-cell proliferation. YM-58483 impedes the proliferation of splenocytes related to MLR by inhibiting the activation of NF-AT[1]. Additionally, it significantly suppresses the production of IL-2 and the promoter activity driven by NF-AT, without affecting the AP-1-driven promoter activity within Jurkat cells[2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 78 mg/mL (185.1 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 78 mg/mL (185.1 mM) |
| 關(guān)鍵字 | inhibit | CRAC Channel | Ca2+ release-activated Ca2+ channels | YM58483 | Calcium release-activated channels | BTP 2 | YM-58483 | BTP-2 | Inhibitor |
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| 相關(guān)庫 | 經(jīng)典已知活性庫 | 疼痛相關(guān)化合物庫 | 神經(jīng)信號分子庫 | 膜蛋白靶向化合物庫 | 神經(jīng)保護(hù)化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 已知活性化合物庫 | 含氟化合物庫 | 離子通道庫 |
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
- Address: 36?Washington?Street, Wellesley?Hills
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