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Postion:Product Catalog >Biochemical Engineering>Inhibitors>GPCR & G Protein>CXCR antagonist>SB225002
SB225002
  • SB225002

SB225002 NEW

Price $43 $61 $129
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-17

Product Details

Product Name: SB225002 CAS No.: 182498-32-4
Purity: 98.79% Supply Ability: 10g
Release date: 2024/11/17

Product Introduction

Bioactivity

名稱SB225002
描述SB225002 is a potent and selective CXCR2 antagonist inhibiting interleukin IL-8 binding to CXCR2.
細(xì)胞實(shí)驗(yàn)Three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit I. Briefly, 1.5 × 103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (antagonist of CXCR2, 400 nM) is added to cells and 0.001% DMSO (solvent) is added as a control. After the indicated incubation period, 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates were left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader.(Only for Reference)
激酶實(shí)驗(yàn)Radioligand Binding Experiments: Assays are performed in 96-well microtiter plates where the reaction mixture contains 1.0 μg/ml membrane protein in 20 mM Bis-Tris-propane, pH 8.0, with 1.2 mM MgSO4, 0.1 mM EDTA, 25 mM NaCl, and 0.03% CHAPS and SB 225002 (10 mM stock in Me2SO) added at the indicated concentrations, the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8 (2,200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine, 0.5% BSA and washed three times with 25 mM NaCl, 10 mM Tris·HCl, 1 mM MgSO4, 0.5 mM EDTA, 0.03% CHAPS, pH 7.4. The filter is dried, sealed in a sample bag containing 10 ml of Wallac 205 Betaplate liquid scintillation fluid, and counted with a Wallac 1205 Betaplate liquid scintillation counter.
體外活性SB225002 demonstrates prolonged analgesic effects and reduces TNBS-induced colitis in mouse models. In rabbits, SB225002 selectively inhibits the margination of neutrophils induced by IL-8. Moreover, at a dosage of 1 mg/kg i.p., SB225002 suppresses the growth of subcutaneously transplanted tumors in a mouse model of intrahepatic cholangiocarcinoma.
體內(nèi)活性SB225002 demonstrates antitumor activity as a microtubule inhibitor. It significantly reduces the levels of phosphorylated ERK1/2 and decreases the proliferation of WHCO1 cells. In vitro, SB225002 inhibits calcium mobilization stimulated by GROα and effectively suppresses the chemotaxis of human and rabbit neutrophils induced by IL-8 and GROα.
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 : 55 mg/mL (156.19 mM)
Ethanol : 3 mg/mL (8.51 mM), Heating is recommended.
關(guān)鍵字SB-225002 | CXC chemokine receptors | CXCR | Inhibitor | inhibit | SB225002 | SB 225002
相關(guān)產(chǎn)品AZD8309 | rac-NBI-74330 | Delmetacin | Tannic acid | Artemotil | CXCR2-IN-1 | LIT927 | Reparixin | Plerixafor octahydrochloride | Nicotinamide N-oxide | Plerixafor | CXCL-CXCR1/2-IN-1
相關(guān)庫(kù)高選擇性抑制劑庫(kù) | 表型篩選靶點(diǎn)鑒定庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 干細(xì)胞分化化合物庫(kù) | 腫瘤免疫治療小分子化合物庫(kù) | 已知活性化合物庫(kù) | GPCR靶點(diǎn)分子庫(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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