B8200-5mg | SB 225002 [182498-32-4] Clinisciences

Background

SB 225002 is a potent and selective CXCR2 chemokine receptor antagonist with IC50 value of 22nM [1].
CXCR2 is a member of the G-protein-coupled receptor family, which is responsible for neutrophil chemotaxis and margination induced by IL-8 [1].
SB 225002 is a potent and selective non-peptide inhibitor of CXCR2. It prevented IL-8 binding to CXCR2 with IC50 value of 22 nM and showed >150-fold selectivity over CXCR1. In HL60 cells, SB 225002 potently prevented IL-8 and GROa-induced neutrophil chemotaxis [1]. In CDDP-resistant and -sensitive OVCA cell lines, SB225002 induced apoptosis in both wild-type and p53-deficient cells in a p53-independent way and promoted mitotic catastrophe [2].
In rabbits, SB 225002 blocked IL-8-induced neutrophil margination [1]. In experimental colitis mice induced by TNBS, SB225002 reduced neutrophil influx, IL-1 , MIP-2, and keratinocyte-derived chemokine (KC) levels, MPO activity and the expression of vascular endothelial growth factor. While, levels of IL-4 and IL-10 were increased significantly in the colons of mice [3].
References:
[1]. White JR, Lee JM, Young PR, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem, 1998, 273(17): 10095-10098.
[2]. Du M, Qiu Q, Gruslin A, et al. SB225002 promotes mitotic catastrophe in chemo-sensitive and -resistant ovarian cancer cells independent of p53 status in vitro. PLoS One, 2013, 8(1): e54572.
[3]. Manjavachi MN, Quintão NL, Campos MM, et al. The effects of the selective and non-peptide CXCR2 receptor antagonist SB225002 on acute and long-lasting models of nociception in mice. Eur J Pain, 2010, 14(1): 23-31.

Product Citation

1. Nureen H Mohamad Zaki, Junya Shiota, et al. "C-X-C motif chemokine ligand 1 induced by Hedgehog signaling promotes mouse extrahepatic bile duct repair after acute injury." Hepatology. 2022 Oct;76(4):936-950. PMID: 35388502
2. Bhattacharya U, Gutter-Kapon L, et al. "Heparanase and Chemotherapy Synergize to Drive Macrophage Activation and Enhance Tumor Growth." Cancer Res. 2020 Jan 1;80(1):57-68. PMID: 31690669

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	352.14
Cas No.	182498-32-4
Formula	C₁₃H₁₀BrN₃O₄
Solubility	insoluble in H2O; ≥15.9 mg/mL in DMSO; ≥6.98 mg/mL in EtOH with ultrasonic
Chemical Name	1-(2-bromophenyl)-3-(2-hydroxy-4-nitrophenyl)urea
SDF	Download SDF
Canonical SMILES	OC1=C(NC(NC2=CC=CC=C2Br)=O)C=CC([N+]([O-])=O)=C1
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity = 97.13%

Chemical structure

SB 225002 [182498-32-4]

Referentie B8200-5mg

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