SCH 527123
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SCH-527123是一种新型的选择性趋化因子受体2（CXCR2）拮抗剂。SCH-527123通过减少NF-κB/MAPK/AKT信号通路的磷酸化，从而抑制CXCR2介导的信号传导[1]。
用浓度逐渐增加的SCH-527123处理细胞72小时，可以剂量依赖性地抑制细胞的生长，IC50值为18-40 μmol/L。然而，与亲代细胞相比，IL-8过表达的细胞展示了更大的IC50值，如在HCT116 和E2细胞中，IC50值 分别为 28.9 ± 0.02 μmol/L和39.5 ± 0.01 μmol/L; 在Caco2和IIIe 细胞中，IC50值 分别为18.8 ± 0.03 μmol/L和25.5 ± 0.02 μmol/L。因此，SCH-527123在结直肠癌细胞系中降低了其生长抑制活性[2]。
参考文献：
[1]. Holz O, Khalilieh S, Ludwig-Sengpiel A et al. SCH527123, a novel CXCR2 antagonist, inhibits ozone-induced neutrophilia in healthy subjects. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al.
[2]. Holz O1, Khalilieh S, Ludwig-Sengpiel A et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. Mol Cancer Ther. 2012 Jun;11(6):1353-64.
- 1. Ravi Holani, Anshu Babbar, et al. "Cathelicidin-mediated lipopolysaccharide signaling via intracellular TLR4 in colonic epithelial cells evokes CXCL8 production." Gut Microbes. 2020 Nov 9;12(1):1785802. PMID:32658599
- 2. Ian Johnston. "Platelet Factor 4 And Von Willebrand Factor Form An Immunogenic, Prothrombotic Complex In Heparin-Induced Thrombocytopenia." University of Pennsylvania.2018.
- 3. Ravi Holani, Fernando Lopes, et al. "Cathelicidin senses enteric pathogen Salmonella typhimurium/LPS for colonic chemokine generation: a new innate immune role for a host defense peptide." bioRxiv. 2018.
- 4. Jinghua Jiang , Fei Ye, et al. "Peri-tumor associated fibroblasts promote intrahepatic metastasis of hepatocellular carcinoma by recruiting cancer stem cells." Cancer Letters.17 July 2017 1/10.
- 5. Khanam A, Trehanpati N, et al. "Blockade of Neutrophil's Chemokine Receptors CXCR1/2 Abrogate Liver Damage in Acute-on-Chronic Liver Failure." Front Immunol. 2017 Apr 24;8:464. PMID:28484461
- 6. Giannou AD, Marazioti A, et al. "NRAS destines tumor cells to the lungs." EMBO Mol Med. 2017 May;9(5):672-686. PMID:28341702
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 397.42 |
| Cas No. | 473727-83-2 |
| Formula | C21H23N3O5 |
| Synonyms | SCH-527123;SCH527123 |
| Solubility | insoluble in H2O; ≥103 mg/mL in EtOH with ultrasonic; ≥19.85 mg/mL in DMSO |
| Chemical Name | 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide |
| SDF | Download SDF |
| Canonical SMILES | CCC(C1=CC=C(O1)C)NC2=C(C(=O)C2=O)NC3=CC=CC(=C3O)C(=O)N(C)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
人黑色素瘤细胞系（A375SM） |
|
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
1 μg/ml；72 h |
|
应用 |
在体外，SCH-479833或SCH527123抑制黑色素瘤细胞的增殖、趋化性和侵袭潜力。SCH-479833或SCH527123处理黑色素瘤细胞也抑制肿瘤生长。组织学和组织化学分析显示，肿瘤中肿瘤细胞的增殖和微血管密度均显著下降（P |
| 动物实验[1]： | |
|
动物模型 |
雄性BALB/c小鼠（20-25 g） |
|
剂量 |
Sch-527123悬浮在0.4％的甲基纤维素中 |
|
应用 |
Sch 527123与小鼠、大鼠和食蟹猴的CXCR2受体具有高亲和性，Kd值分别为0.20 nM、0.20 nM和0.08 nM。Sch 527123是一种有效的CXCR2介导趋化性的拮抗剂，IC50值约为3-6 nM。相比之下，Sch 527123与食蟹猴CXCR1具有较低的亲和力，Kd值为41 nM，仅能较弱抑制食蟹猴CXCR1介导的趋化性，IC50值约为1000 nM。在鼻内给药脂多糖（LPS）的小鼠中，Sch-527123口服给药可以阻断肺中性粒细胞增多（ED50=1.2 mg/kg）和杯状细胞增生（在1-3 mg/kg时抑制32-38%）。在大鼠中，Sch-527123抑制气管内（i.t.）LPS诱导的肺中性粒细胞增多（ED=501.8 mg/kg）和支气管肺泡灌洗（BAL）粘蛋白含量的增加（ED50≤ 0.1 mg/kg）。在气管内（i.t.）五氧化二钒（vanadium pentoxide）给药的大鼠中，Sch-527123也抑制肺中性粒细胞增多（ED50=1.3 mg/kg）、杯状细胞增生（ED 50=0.7 mg/kg）和BAL粘蛋白含量的增加（ED50 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1. Singh S1, Sadanandam A, Nannuru KC et al. Small-molecule antagonists for CXCR2 and CXCR1 inhibit human melanoma growth by decreasing tumor cell proliferation, survival, and angiogenesis. Clin Cancer Res. 2009 Apr 1;15(7):2380-6. 2. Chapman RW1, Minnicozzi M, Celly CS et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93. Epub 2007 May 11. |
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| 描述 | SCH-527123是一种有效的CXCR1和CXCR2拮抗剂，IC50值分别为42 nM和3 nM。 | |||||
| 靶点 | CXCR1 | CXCR2 | ||||
| IC50 | 42 nM | 3 nM | ||||
质量控制和MSDS
- 批次：
化学结构
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