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SB225002

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Chemical Structure| 182498-32-4 同义名 : -
CAS号 : 182498-32-4
货号 : A149514
分子式 : C13H10BrN3O4
纯度 : 99%+
分子量 : 352.14
MDL号 : MFCD00954637
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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

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]
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
实验方案
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
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.