SB225002

製品コードS7651 バッチS765101

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C13H10BrN3O4
分子量 352.14 CAS No. 182498-32-4
Solubility (25°C)* 体外 DMSO 70 mg/mL (198.78 mM)
Ethanol 3 mg/mL warmed with 50ºC water bath (8.51 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
in vitro In vitro, SB225002 inhibits GROα-stimulated calcium mobilization, and potently inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROalpha. [1] SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. [2] SB225002 also shows the antitumor activity as a microtubule inhibitor. [3]
in vivo In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. [1] In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. [4] In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models. [5] [6]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 WHCO1, WHCO5, and WHCO6 cell lines
濃度 400 nM
反応時間 6 days
実験の流れ 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.
動物実験 動物モデル Rabbits
投薬量 5.5 μg/kg/min
投与方法 Cannula in the external jugular vein

カスタマーフィードバック

, , J Cell Mol Med, 2017, 21(7):1411-1419

, , Mol Pain, 2016, doi: 10.1177/1744806916646381

Data from [Data independently produced by , , Theranostics, 2018, 8(5):1270-1285]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Extracellular-vesicle-packaged S100A11 from osteosarcoma cells mediates lung premetastatic niche formation by recruiting gMDSCs [ Cell Rep, 2024, 43(2):113751] PubMed: 38341855
Oncogenic KRASG12D extrinsically induces an immunosuppressive microenvironment in lung adenocarcinoma [ bioRxiv, 2024, 2024.01.16.568090] PubMed: 38293141
PMN-MDSCs modulated by CCL20 from cancer cells promoted breast cancer cell stemness through CXCL2-CXCR2 pathway [ Signal Transduct Target Ther, 2023, 8(1):97] PubMed: 36859354
Tumor Cell-Intrinsic SETD2 Deficiency Reprograms Neutrophils to Foster Immune Escape in Pancreatic Tumorigenesis [ Adv Sci (Weinh), 2023, 10(2):e2202937] PubMed: 36453584
Surgical Treatment of Osteosarcoma Induced Distant Pre-Metastatic Niche in Lung to Facilitate the Colonization of Circulating Tumor Cells [ Adv Sci (Weinh), 2023, 10(28):e2207518] PubMed: 37585564
Surgical Treatment of Osteosarcoma Induced Distant Pre-Metastatic Niche in Lung to Facilitate the Colonization of Circulating Tumor Cells [ Adv Sci (Weinh), 2023, 10(28):e2207518] PubMed: 37585564
Sepsis induces non-classic innate immune memory in granulocytes [ Cell Rep, 2023, 42(9):113044] PubMed: 37643085
A precise molecular subtyping of ulcerative colitis reveals the immune heterogeneity and predicts clinical drug responses [ J Transl Med, 2023, 21(1):466] PubMed: 37443022
Microbial-Dependent Recruitment of Immature Myeloid Cells Promotes Intestinal Regeneration [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007] PubMed: 37898454
Blocking the CXCL1-CXCR2 axis enhances the effects of doxorubicin in HCC by remodelling the tumour microenvironment via the NF-κB/IL-1β/CXCL1 signalling pathway [ Cell Death Discov, 2023, 9(1):120] PubMed: 37037815

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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