SB225002 | CXCR2 Antagonist | AmBeed-信号通路专用抑制剂

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SB225002 {[allProObj[0].p_purity_real_show]}

货号：A149514

SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM, showing > 150-fold selectivity over CXCR1 and four other 7-TMRs.

SB225002 化学结构
CAS号：182498-32-4

SB225002 3D分子结构
CAS号：182498-32-4

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SB225002 纯度/质量文件产品仅供科研

货号：A149514 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

CXCR 亚型比较

产品名称	CXCR1 ↓ ↑	CXCR2 ↓ ↑	CXCR4 ↓ ↑	纯度
Reparixin	✔			99%+
SB225002		+++ CXCR2, IC50: 22 nM		99%+
Plerixafor			++ CXCR4, IC50: 44 nM	99%
AMD 3465 6HBr			✔	98%
WZ811			++++ CXCR4, EC50: 0.3 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SB225002 生物活性

靶点	CXCR2 CXCR2, IC50:22 nM
描述	CXCR2 is expressed in human neutrophilsand a subset of T-cells, which can mediate neutrophil migration to sites of inflammation through binding with and internalization through its ligand IL-8 or related chemokines containing a common amino-terminal ELR amino acid sequence (Glu-Leu-Arg), such as GROα, GROβ, GROγ, NAP-2 and ENA-78. SB 225002 is a non-peptide, potent and selective CXCR2 inhibitor with IC50 value of 22 nM, >150-fold selectivity over CXCR1 and four other 7-TMRs tested. SB-225002 can produce a dose-dependent inhibition of calcium mobilization induced by IL-8 and GROα with IC50 values of 8 nM and 10 nM, respectively, in differentiated HL60 cells with predominantly express CXCR2 (80%) with a much smaller number of CXCR1 (20%) receptors, as well as inhibit both IL-8 (1nM)- and GROα (10nM)-mediated human neutrophil chemotaxis with IC50s of 20 nM and 60 nM, respectively. This effect of SB-225002 on chemotaxis can also be observed in in vivo study^[1]. Daily intraperitoneal injection with SB225002 at dose of 5 mg/kg for 4 weeks showed significantly tumor growth inhibition by ~45% decrease in tumor size of LLC tumor bearing GRK6-/- mice.
作用机制	SB-225002 can inhibit CXCR2 through competition with IL-8.^[1]

SB225002 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
CHO cells		Function assay		Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells, IC50=22 nM	17236763
HEK293 cells		Function assay		Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=40 nM	25254640
human PMNs		Function assay		Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=30 nM	25254640

SB225002 动物研究

Dose	Mice: 0.3 mg/kg - 1 mg/kg^[3] (i.p.), 4 mg/kg^[4] (i.p.)
Administration	i.p.

SB225002 参考文献

[1]White JR, Lee JM, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.

[2]Raghuwanshi SK, Smith N, et al. G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis. J Immunol. 2013 May 15;190(10):5329-36.

SB225002 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.84mL

0.57mL

0.28mL

14.20mL

2.84mL

1.42mL

28.40mL

5.68mL

2.84mL

SB225002 技术信息

CAS号	182498-32-4
分子式	C₁₃H₁₀BrN₃O₄
分子量	352.14

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(298.18 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+35% PEG300+water 2.5 mg/mL clear

PO 0.5% CMC-Na 41 mg/mL suspension

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

CHO cells	Function assay	Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells, IC50=22 nM	17236763
HEK293 cells	Function assay	Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=40 nM	25254640
human PMNs	Function assay	Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=30 nM	25254640

SB225002 {[allProObj[0].p_purity_real_show]}

SB225002 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SB225002 质控信息

SB225002 生物活性

SB225002 细胞研究

SB225002 动物研究

SB225002 参考文献

SB225002 实验方案

SB225002 技术信息

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SB225002 {[allProObj[0].p_purity_real_show]}

SB225002 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SB225002 质控信息

SB225002 生物活性

SB225002 细胞研究

SB225002 动物研究

SB225002 参考文献

SB225002 实验方案

SB225002 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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SB225002 纯度/质量文件产品仅供科研