[CAS NO. 182498-32-4] SB225002

Name: SB225002
Brand: Arctom Scientific
SKU: SLK-S7651

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PRODUCTS SPECIFICATIONS [182498-32-4]

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Catalog

SLK-S7651

Brand

Selleck

CAS

182498-32-4

DESCRIPTION [182498-32-4]

Overview

MDL	MFCD00954637
Molecular Weight	352.14
Molecular Formula	C13H10BrN3O4
SMILES	O=C(NC1=CC=C([N+]([O-])=O)C=C1O)NC2=CC=CC=C2Br

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.8398 mL	14.1989 mL	28.3978 mL
5 mM	0.5680 mL	2.8398 mL	5.6796 mL
10 mM	0.2840 mL	1.4199 mL	2.8398 mL
50 mM	0.0568 mL	0.2840 mL	0.5680 mL

Description

SB225002 is a potent, and selective antagonist with of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

Targets

CXCR2 ^[1]
(Cell-free assay)

22 nM

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. SB 225002 substantially reduces the levels of phosphorylated ERK1/2, and decreases cell proliferation in WHCO1 cells. SB225002 also shows the antitumor activity as a microtubule inhibitor.

In vivo

In rabbits, SB225002 selectively blocks IL-8-induced neutrophil margination. In mouse intrahepatic cholangiocellular carcinoma model, SB225002 (1 mg/kg i.p.) suppresses the growth of transplanted subcutaneous tumors. In addition, SB225002 also displays long-lasting antinociceptive effects, and reduces TNBS-induced colitis in mouse models.

References

[1] White JR, et al. J Biol Chem. 1998, 273(17), 10095-10098.
[2] Wang B, et al. Cancer Res. 2006, 66(6), 3071-3077.
[3] Goda AE, et al. Biochem Pharmacol. 2013, 85(12), 1741-1752.
[4] Sueoka H, et al. Surgery. 2014, 155(4), 640-649.
[5] Manjavachi MN, et al. Eur J Pain. 2010, 14(1), 23-31.
[6] Bento AF, et al. J Leukoc Biol. 2008, 84(4), 1213-1221.