SB225002
Based on 65 publication(s) in Google Scholar
SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 182498-32-4
- Formula: C13H10BrN3O4
- Molecular Weight:352.14
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) SB225002
More- Cancer Discov. 2026 Apr 8. [Abstract]
- Bioact Mater. 2021 Jan 7;6(7):2039-2057. [Abstract]
- Cell Host Microbe. 2025 Jun 11;33(6):915-931.e9. [Abstract]
- Cancer Res. 2018 Oct 1;78(19):5586-5599. [Abstract]
- Nat Commun. 2024 Oct 14;15(1):8845. [Abstract]
- Nat Commun. 2022 Nov 26;13(1):7281. [Abstract]
- Nat Commun. 2020 Feb 28;11(1):1126. [Abstract]
- Sci Transl Med. 2026 May 27;18(851):eadv8372. [Abstract]
- Adv Sci (Weinh). 2026 Jun 22:e76195. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(24):e19500. [Abstract]
- Adv Sci (Weinh). 2025 Oct 28:e16569. [Abstract]
- Adv Sci (Weinh). 2025 May 28:e01011. [Abstract]
- Adv Sci (Weinh). 2025 Jan 22:e2414779. [Abstract]
- Adv Sci (Weinh). 2023 Nov;10(33):e2302498. [Abstract]
- J Adv Res. 2024 Aug 19:S2090-1232(24)00366-7. [Abstract]
- Exp Mol Med. 2022 Nov;54(11):2022-2035. [Abstract]
- Sci Adv. 2025 Aug 22;11(34):eadw6926. [Abstract]
- Redox Biol. 2024 Aug:74:103209. [Abstract]
- Cell Rep Med. 2026 Mar 17;7(3):102635. [Abstract]
- Pharmacol Res. 2026 May:227:108169. [Abstract]
- Cancer Lett. 2023 Aug 28:570:216330. [Abstract]
- Mol Biomed. 2021 Dec 5;2(1):37. [Abstract]
- Int J Biol Sci. 2022 Jan 9;18(3):1271-1287. [Abstract]
- Cell Death Dis. 2026 Feb 2;17(1):197. [Abstract]
- Adv Healthc Mater. 2025 Sep 30:e01619. [Abstract]
- Dev Cell. 2026 Jan 12:S1534-5807(25)00768-3. [Abstract]
- Int J Biol Macromol. 2024 Jun;269(Pt 2):132025. [Abstract]
- Acta Pharmacol Sin. 2025 Oct 1. [Abstract]
- Cancer Immunol Res. 2026 Jul 2;14(7):1172-1185. [Abstract]
- Apoptosis. 2026 May 24;31(6):152. [Abstract]
- Clin Sci. 2026 Feb 11;140(2):201-219. [Abstract]
- Mucosal Immunol. 2025 Mar 28:S1933-0219(25)00031-5. [Abstract]
- Brain Behav Immun. 2023 Mar:109:308-320. [Abstract]
- Brain Behav Immun. 2022 May:102:23-39. [Abstract]
- JHEP Rep. 2025 Mar 7;7(6):101385. [Abstract]
- J Autoimmun. 2018 May:89:30-40. [Abstract]
- Cell Rep. 2024 Apr 23;43(4):114088. [Abstract]
- JCI Insight. 2025 Nov 25:e196605. [Abstract]
- JCI Insight. 2022 Aug 23;e155296. [Abstract]
- Cancer Cell Int. 2023 Oct 11;23(1):237. [Abstract]
- Cell Biol Toxicol. 2025 Oct 24;41(1):143. [Abstract]
- J Mol Cell Biol. 2023 Aug 3;15(4):mjad025. [Abstract]
- Neurobiol Dis. 2024 Dec:203:106744. [Abstract]
- J Ethnopharmacol. 2022 Sep 15:295:115277. [Abstract]
- Int J Mol Sci. 2023 Jun 21;24(13):10432. [Abstract]
- Pharmaceuticals (Basel). 2025 Oct 14;18(10):1547. [Abstract]
- Neuropharmacology. 2018 Jun:135:34-47. [Abstract]
- Cancers (Basel) . 2024 Jul 30;16(15):2714. [Abstract]
- Lipids Health Dis. 2022 Dec 29;21(1):147. [Abstract]
- J Dermatol Sci. 2022 Nov;108(2):98-108. [Abstract]
- J Cell Physiol. 2021 Apr;236(4):3114-3128. [Abstract]
- ACS Pharmacol Transl Sci. 2024 Apr 18;7(5):1533-1545. [Abstract]
- Cytokine. 2022 Mar:151:155789. [Abstract]
- J Immunol Res. 2022 Jul 16:2022:7966089. [Abstract]
- Mol Med Rep. 2019 Aug;20(2):1065-1074. [Abstract]
- Mol Immunol. 2018 Sep:101:440-449. [Abstract]
- Discov Oncol. 2024 Nov 2;15(1):614. [Abstract]
- Exp Biol Med. 2020 Mar;245(6):562-575. [Abstract]
- bioRxiv. 2025 Dec 1:2025.11.26.690859. [Abstract]
- State University of New York. 2025.
- Patent. US20250123282A1.
- Res Sq. 2024 Jun 19.
- Int J Biol Sci. 2022 Jan 16;18(4):1363-1380. [Abstract]
- Research Square Preprint. 2021 Aug.
- Research Square Preprint. 2020 Oct.
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
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Flow Cytometry
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IF
Biological Activity
|
125I-IL-8-CXCR2 22 nM (IC50, in CHO cell membrane) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | IC50 |
100 μM
Compound: 65; SB225002
|
Antiproliferative activity against human 786-0 cells
Antiproliferative activity against human 786-0 cells
|
[PMID: 38278080] |
| A498 | IC50 |
70 μM
Compound: 65; SB225002
|
Antiproliferative activity against human A498 cells
Antiproliferative activity against human A498 cells
|
[PMID: 38278080] |
| CHO | IC50 |
0.5 μM
Compound: 2, SB-225002
|
Antagonist activity at CXCR2 expressed in 7w CHO cells co-expressing human recombinant APP 751 assessed as inhibition of gamma-secretase-mediated amyloid beta42 production
Antagonist activity at CXCR2 expressed in 7w CHO cells co-expressing human recombinant APP 751 assessed as inhibition of gamma-secretase-mediated amyloid beta42 production
|
[PMID: 19853461] |
| CHO | IC50 |
22 nM
Compound: Table 1 C5R13
|
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells
|
[PMID: 17236763] |
| HEK293 | IC50 |
40 nM
Compound: 2, SB225002
|
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux 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
|
[PMID: 25254640] |
SB225002 (SB 225002) is an antagonist of 125I-IL-8 binding to CXCR2 with an IC50=22 nM. SB225002 shows >150-fold selectivity over CXCR1 and four other 7-TMRs tested. SB225002 is a potent antagonist of rabbit CXCR2, inhibiting rabbit PMN chemotaxis in response to optimal concentrations of human IL-8 or GROα (IC50 values of 30 and 70 nM, respectively. In these cells (PMN, HL60, CXCR1-RBL-2H3), SB225002 produces a concentration-dependent inhibition of both IL-8- and GROα-mediated calcium mobilization with IC50 values of 8 and 10 nM, respectively. In 3ASubE cells stably transfected with CXCR2, SB 225002 dose-dependently inhibits calcium mobilization induced by both GROα and IL-8, with IC50 values of 20 and 40 nM, respectively[1]. WHCO1 cells treated with SB225002 exhibits a 40% reduction in cell proliferation. Blocking CXCR2 signaling in WHCO1 cells with 400 nM SB225002 (SB 225002) significantly decreases cell proliferation by ~40% to 50%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 182498-32-4
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Appearance Solid
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Molecular Weight 352.14
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Formula C13H10BrN3O4
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C([N+]([O-])=O)C=C1O)NC2=CC=CC=C2Br
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)
Publications (65)
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Journal Impact Factor
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Most Recent
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Cancer Discov
Arachidonic Acid Metabolism in PMN-MDSCs Suppresses Antitumor Capacity of T cells in KRAS-Mutant Cholangiocarcinoma. [Abstract]2026 Apr 8. PMID: 41949259 -
Bioact Mater
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering. [Abstract]2021 Jan 7;6(7):2039-2057. PMID: 33511306 -
Cell Host Microbe
Microbiota-derived urocanic acid triggered by tyrosine kinase inhibitors potentiates cancer immunotherapy efficacy. [Abstract]2025 Jun 11;33(6):915-931.e9. PMID: 40441145 -
Cancer Res
A RIPK3-PGE2 Circuit Mediates Myeloid-Derived Suppressor Cell-Potentiated Colorectal Carcinogenesis. [Abstract]2018 Oct 1;78(19):5586-5599. PMID: 30012671 -
Nat Commun
Non-homogenous intratumor ionizing radiation doses synergize with PD1 and CXCR2 blockade. [Abstract]2024 Oct 14;15(1):8845. PMID: 39397001
SB225002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 14;15(1):8845. [Abstract]
SB225002 was administered i.p. at 10 mg/kg after SBRT, and every day for 8 days. Kaplan–Meier survival curves of the efficacy experiment were generated.
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Nat Commun
ARID1A loss induces polymorphonuclear myeloid-derived suppressor cell chemotaxis and promotes prostate cancer progression. [Abstract]2022 Nov 26;13(1):7281. PMID: 36435834
SB225002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 26;13(1):7281. [Abstract]
SB225002 (2 mg/kg) in DMSO was diluted in corn oil for in vivo administration through intraperitoneal injection every other day or gavage daily, respectively. Mice were inoculated with WT or Arid1a KO Myc-CaP cells and treated with or without SB225002. Quantification of each tumor-infiltrating immune cell population. was measured by FACS analysis.
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Nat Commun
Chemotaxis-driven delivery of nano-pathogenoids for complete eradication of tumors post-phototherapy. [Abstract]2020 Feb 28;11(1):1126. PMID: 32111847 -
Sci Transl Med
CCR5 and CD74 are potential therapeutic targets for necroinflammation in preclinical cholesterol crystal embolism. [Abstract]2026 May 27;18(851):eadv8372. PMID: 42202044 -
Adv Sci (Weinh)
Neuron-Derived MIF Engages VCAM1 to Fuel a Self-Amplifying CXCL8 Loop That Drives Perineural Invasion and Metastasis in Gastric Cancer. [Abstract]2026 Jun 22:e76195. PMID: 42330341 -
Adv Sci (Weinh)
Diabetes Mellitus Facilitates Gallstone Formation Through CXCR2-NETs-Mediated Liver-Bile Barrier Damage. [Abstract]2026 Apr;13(24):e19500. PMID: 41698066 -
Adv Sci (Weinh)
Repurposing of Chemokine Antagonists for Combined Phase-Resolved Spinal Cord Injury Treatment. [Abstract]2025 Oct 28:e16569. PMID: 41147460 -
Adv Sci (Weinh)
Single-Cell Analysis Reveals that Vitamin C Inhibits Bone Metastasis of Renal Cancer via Cell Cycle Arrest and Microenvironment Remodeling. [Abstract]2025 May 28:e01011. PMID: 40433925 -
Adv Sci (Weinh)
Therapeutic Black Phosphorus Nanosheets Elicit Neutrophil Response for Enhanced Tumor Suppression. [Abstract]2025 Jan 22:e2414779. PMID: 39840467 -
Adv Sci (Weinh)
Tumor Microenvironment Responsive CD8+ T Cells and Myeloid-Derived Suppressor Cells to Trigger CD73 Inhibitor AB680-Based Synergistic Therapy for Pancreatic Cancer. [Abstract]2023 Nov;10(33):e2302498. PMID: 37867243
SB225002 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Nov;10(33):e2302498. [Abstract]
5 mg/kg SB225002 was administered twice a week alone or in combination by intraperitoneal injection according to the experimental objective. A schematic representation of the therapy schedule for AB680, anti-PD-1 antibody, and CXCR2 inhibitor SB225002 in the KPC orthotopic model was shown. The images of KPC orthotopic allografts from the Control, SB225002, anti-PD-1+AB680, and combination groups were shown.
SB225002 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Nov;10(33):e2302498. [Abstract]
5 mg/kg SB225002 twice a week alone or in combination by intraperitoneal injection according to the experimental objective The percentages of total CD8+ T cells, Granzyme B+ cells among the total CD8+ T cells, and CXCR2+ MDSCs in the tumors of each group at the endpoint were determined by flow cytometry.
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J Adv Res
Dialog between mantle cell lymphoma cells and lymphoma-associated macrophages underlies ibrutinib resistance. [Abstract]2024 Aug 19:S2090-1232(24)00366-7. PMID: 39168245 -
Exp Mol Med
Protective effect of hepatocyte-enriched lncRNA-Mir122hg by promoting hepatocyte proliferation in acute liver injury. [Abstract]2022 Nov;54(11):2022-2035. PMID: 36424455 -
Sci Adv
Liver regeneration-associated hepatocellular YAP1 activation prevents colorectal cancer liver metastasis through glutamine competition. [Abstract]2025 Aug 22;11(34):eadw6926. PMID: 40845109 -
Redox Biol
Lactate-induced activation of tumor-associated fibroblasts and IL-8-mediated macrophage recruitment promote lung cancer progression. [Abstract]2024 Aug:74:103209. PMID: 38861833 -
Cell Rep Med
Enhancing gastric cancer immunotherapy: Insights from multi-omics analysis and innovations in photodynamic-chemotherapy nanoplatforms. [Abstract]2026 Mar 17;7(3):102635. PMID: 41747719 -
Pharmacol Res
2026 May:227:108169. PMID: 41871675 -
Cancer Lett
Inducible nitric oxide synthase (iNOS)-activated Cxcr2 signaling in myeloid cells promotes TGFβ-dependent squamous cell carcinoma lung metastasis. [Abstract]2023 Aug 28:570:216330. PMID: 37524225 -
Mol Biomed
Cholesterol modified DP7 and pantothenic acid induce dendritic cell homing to enhance the efficacy of dendritic cell vaccines. [Abstract]2021 Dec 5;2(1):37. PMID: 35006477 -
Int J Biol Sci
CXCR4-dependent macrophage-to-fibroblast signaling contributes to cardiac diastolic dysfunction in heart failure with preserved ejection fraction. [Abstract]2022 Jan 9;18(3):1271-1287. PMID: 35173552 -
Cell Death Dis
p16-mediated G0/G1 cell cycle arrest leads to SASP and fibrosis in Fuchs endothelial corneal dystrophy. [Abstract]2026 Feb 2;17(1):197. PMID: 41629264 -
Adv Healthc Mater
Trans-Organ Early Intervention for Myocardial Infarction Based on Bone Marrow-Homing Biomimetic Nanomedicine. [Abstract]2025 Sep 30:e01619. PMID: 41025748 -
Dev Cell
MITA/STING-driven CD38 induction in Siglec-Flow macrophages promotes regulatory T cell survival and non-small cell lung cancer progression. [Abstract]2026 Jan 12:S1534-5807(25)00768-3. PMID: 41529690 -
Int J Biol Macromol
2024 Jun;269(Pt 2):132025. PMID: 38704076 -
Acta Pharmacol Sin
HDAC inhibitor GCJ-490A modulates tumor microenvironment and synergizes with PD-1 antibody against breast and lung cancers in syngeneic murine models. [Abstract]2025 Oct 1. PMID: 41034396 -
Cancer Immunol Res
Tumor-Derived Complement C3 Overexpression in STK11-Mutant Lung Adenocarcinoma Drives Tumor Growth and Immune Checkpoint Inhibitor Resistance. [Abstract]2026 Jul 2;14(7):1172-1185. PMID: 42048614 -
Apoptosis
Neutrophil extracellular traps in post-traumatic urethral microenvironment promote hypertrophic urethral stricture via the TLR9/NF-kB/Smad3/IL-8 axis. [Abstract]2026 May 24;31(6):152. PMID: 42178452 -
Clin Sci
Evaluation of inflammation-mediated cancer progression during FLASH and conventional irradiation-induced lung injury. [Abstract]2026 Feb 11;140(2):201-219. PMID: 41552931 -
Mucosal Immunol
Single-cell sequencing reveals the same heterogeneity of neutrophils in heatstroke-induced lung and liver injury. [Abstract]2025 Mar 28:S1933-0219(25)00031-5. PMID: 40158777 -
Brain Behav Immun
Schwann cell-derived CXCL2 contributes to cancer pain by modulating macrophage infiltration in a mouse breast cancer model. [Abstract]2023 Mar:109:308-320. PMID: 36754246 -
Brain Behav Immun
Spinal microglia-derived TNF promotes the astrocytic JNK/CXCL1 pathway activation in a mouse model of burn pain. [Abstract]2022 May:102:23-39. PMID: 35143878 -
JHEP Rep
Proinflammatory macrophages release CXCL5 to regulate T cell function and limit effects of αPD-1 in steatosis-driven liver cancer. [Abstract]2025 Mar 7;7(6):101385. PMID: 40496444 -
J Autoimmun
Decrease of galectin-3 in keratinocytes: A potential diagnostic marker and a critical contributor to the pathogenesis of psoriasis. [Abstract]2018 May:89:30-40. PMID: 29167025
SB225002 purchased from MedChemExpress. Usage Cited in: J Autoimmun. 2018 May:89:30-40. [Abstract]
The blockade of neutrophil infiltration and intracutaneous injection of exogenous galectin-3 ameliorates skin inflammation in galectin 3-/- mice
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Cell Rep
IFNα-induced BST2+ tumor-associated macrophages facilitate immunosuppression and tumor growth in pancreatic cancer by ERK-CXCL7 signaling. [Abstract]2024 Apr 23;43(4):114088. PMID: 38602878 -
JCI Insight
ANGPTL8 links refeeding to monocyte dynamics and metabolic inflammation via the CCL5-CCR5 axis. [Abstract]2025 Nov 25:e196605. PMID: 41289013 -
JCI Insight
2022 Aug 23;e155296. PMID: 35998057 -
Cancer Cell Int
A novel STAT3/ NFκB p50 axis regulates stromal-KDM2A to promote M2 macrophage-mediated chemoresistance in breast cancer. [Abstract]2023 Oct 11;23(1):237. PMID: 37821959 -
Cell Biol Toxicol
ATG5-dependent autophagy in Sertoli cells protects against cadmium-disrupted blood-testis barrier via perturbing CXCL2/CXCR2 axis. [Abstract]2025 Oct 24;41(1):143. PMID: 41131418 -
J Mol Cell Biol
CSF2 upregulates CXCL3 expression in adipocytes to promote metastasis of breast cancer via the FAK signaling pathway. [Abstract]2023 Aug 3;15(4):mjad025. PMID: 37073091 -
Neurobiol Dis
2024 Dec:203:106744. PMID: 39603278 -
J Ethnopharmacol
Feiyanning downregulating CXCLs/CXCR2 axis to suppress TANs infiltration in the prevention of lung cancer metastasis. [Abstract]2022 Sep 15:295:115277. PMID: 35427725 -
Int J Mol Sci
C-X-C Motif Chemokine 3 Promotes the Inflammatory Response of Microglia after Escherichia coli-Induced Meningitis. [Abstract]2023 Jun 21;24(13):10432. PMID: 37445610 -
Pharmaceuticals (Basel)
Direct Targeting of CXCR2 Receptor Inhibits Neuroblastoma Growth: An In Vitro Assessment. [Abstract]2025 Oct 14;18(10):1547. PMID: 41155662 -
Neuropharmacology
Levo-corydalmine alleviates vincristine-induced neuropathic pain in mice by inhibiting an NF-kappa B-dependent CXCL1/CXCR2 signaling pathway. [Abstract]2018 Jun:135:34-47. PMID: 29518397 -
Cancers (Basel)
Evaluation of the Mammalian Aquaporin Inhibitors Auphen and Z433927330 in Treating Breast Cancer. [Abstract]2024 Jul 30;16(15):2714. PMID: 39123442 -
Lipids Health Dis
Exosomal IL-8 derived from Lung Cancer and Colon Cancer cells induced adipocyte atrophy via NF-κB signaling pathway. [Abstract]2022 Dec 29;21(1):147. PMID: 36581870 -
J Dermatol Sci
Uncoupling melanogenesis from proliferation in epidermal melanocytes responding to stimulation with psoriasis-related proinflammatory cytokines. [Abstract]2022 Nov;108(2):98-108. PMID: 36577564 -
J Cell Physiol
IL-8/CXCR2 mediates tropism of human bone marrow-derived mesenchymal stem cells toward CD133+ /CD44+ Colon cancer stem cells. [Abstract]2021 Apr;236(4):3114-3128. PMID: 33078417 -
ACS Pharmacol Transl Sci
Development of a Fluorescent Ligand for the Intracellular Allosteric Binding Site of the Neurotensin Receptor 1. [Abstract]2024 Apr 18;7(5):1533-1545. PMID: 38751637 -
Cytokine
2022 Mar:151:155789. PMID: 34998158 -
J Immunol Res
CXCR2 Is Essential for Radiation-Induced Intestinal Injury by Initiating Neutrophil Infiltration. [Abstract]2022 Jul 16:2022:7966089. PMID: 35879949 -
Mol Med Rep
2019 Aug;20(2):1065-1074. PMID: 31173199 -
Mol Immunol
Interleukin 8 (CXCL8)-CXC chemokine receptor 2 (CXCR2) axis contributes to MiR-4437-associated recruitment of granulocytes and natural killer cells in ischemic stroke. [Abstract]2018 Sep:101:440-449. PMID: 30096583 -
Discov Oncol
Mechanism of CXCL8 regulation of methionine metabolism to promote angiogenesis in gliomas. [Abstract]2024 Nov 2;15(1):614. PMID: 39488622 -
Exp Biol Med
Mesenchymal stem cells maintain the stemness of colon cancer stem cells via interleukin-8/mitogen-activated protein kinase signaling pathway. [Abstract]2020 Mar;245(6):562-575. PMID: 32122165 -
bioRxiv
Osteoblasts Exert a Pro-Tumorigenic Effect on Breast Cancer Spheroids Through CXCL5/CXCR2 Signaling In 2D And 3D Bone Mimetic Cultures. [Abstract]2025 Dec 1:2025.11.26.690859. PMID: 41394723 -
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Int J Biol Sci
Cancer-associated adipocytes promote the invasion and metastasis in breast cancer through LIF/CXCLs positive feedback loop. [Abstract]2022 Jan 16;18(4):1363-1380. PMID: 35280694 -
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (283.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 25 mg/mL (70.99 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
CHO-CXCR1 and CHO-CXCR2 membranes are prepared. Assays are performed in 96-well microtiter plates where the reaction mixture contained 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane, pH 8.0, with 1.2 mM MgSO4, 0.1 mM EDTA, 25 mM NaCl, and 0.03% CHAPS and SB 225002 (10 mM stock in Me2SO) added at the indicated concentrations, the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8 (2,200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine, 0.5% BSA and washed three times with 25 mM NaCl, 10 mM Tris•HCl, 1 mM MgSO4, 0.5 mMEDTA, 0.03% CHAPS, pH 7.4. The filter is dried, sealed in a sample bag containing 10 mL of Wallac 205 Betaplate liquid scintillation fluid, and counted with a Wallac 1205 Betaplate liquid scintillation counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit. Briefly, 1.5×103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (400 nM) is added to cells and 0.001% DMSO (solvent) is added as a control. After the indicated incubation period, 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates are left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
Male 7-8 weeks old wildtype (C57BL/6J, Harlan) and ApoE−/− mice, which are generated on the same C57BL/6 background, are either fed with a normal chow or a cholesterol rich chow for 6 weeks and submitted to 20 min of left-sided middle cerebral artery occlusion (MCAO) or sham surgery. Animals are randomly attributed to treatment paradigms, and experimenters are blinded at all stages of interventions and data analysis. The selective CXCR2 antagonist SB225002 (2 mg/kg) or vehicle (1% DMSO in PBS) is injected intraperitoneally (i.p.) at 0, 24 and 48 hours post-ischemia. In other experiments, CXCR2 is specifically blocked by i.p. injection of a neutralizing rabbit anti-CXCR2 serum (300 μL) at 0 hours, 24 hours and 48 hours post-ischemia. In the latter studies, normal rabbit serum (NRS) served as control. In some experiments, neutrophils are depleted by i.p. injection of 200 μg anti-mouse Ly6G 24 hours before and 24 hours after ischemia. In these experiments, 200 μg of an isotype control antibody is delivered as control.
Rats[4]
In this study, 10-12 Sprague-Dawley rat pups per dam are used. The pups receive intraperitoneal injections of SB225002 (1 or 3 mg/kg, diluted in NS containing 0.33 % Tween 80) or vehicle (NS solution containing 0.33 % Tween 80) 30 min before lipopolysaccharide (LPS) administration and immediately after hypoxic ischemia (HI). The pups are randomly assigned to four groups: control (pups unexposed to LPS or HI, N=14), vehicle (NS injections 30 min before LPS administration and immediately after HI, N=18), and SB-1 (1 mg/kg, N=14) and SB-3 (3 mg/kg, N=18) (SB225002 injections 30 min before LPS administration and immediately after HI).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. White JR, 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. [Content Brief]
[2]. Wang B, et al. A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer. Cancer Res. 2006 Mar 15;66(6):3071-7. [Content Brief]
[3]. Herz J, et al. Role of Neutrophils in Exacerbation of Brain Injury After Focal Cerebral Ischemia in Hyperlipidemic Mice. Stroke. 2015 Oct;46(10):2916-25. [Content Brief]
[4]. Wang LY, et al. CXCL5 signaling is a shared pathway of neuroinflammation and blood-brain barrier injury contributing to white matter injury in the immature brain. J Neuroinflammation. 2016 Jan 6;13:6. [Content Brief]
[5]. Shi ZR, et al. Decrease of galectin-3 in keratinocytes: A potential diagnostic marker and a critical contributor to the pathogenesis of psoriasis. J Autoimmun. 2018 May;89:30-40. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8398 mL | 14.1989 mL | 28.3978 mL | 70.9945 mL |
| 5 mM | 0.5680 mL | 2.8398 mL | 5.6796 mL | 14.1989 mL | |
| 10 mM | 0.2840 mL | 1.4199 mL | 2.8398 mL | 7.0994 mL | |
| 15 mM | 0.1893 mL | 0.9466 mL | 1.8932 mL | 4.7330 mL | |
| 20 mM | 0.1420 mL | 0.7099 mL | 1.4199 mL | 3.5497 mL | |
| 25 mM | 0.1136 mL | 0.5680 mL | 1.1359 mL | 2.8398 mL | |
| 30 mM | 0.0947 mL | 0.4733 mL | 0.9466 mL | 2.3665 mL | |
| 40 mM | 0.0710 mL | 0.3550 mL | 0.7099 mL | 1.7749 mL | |
| 50 mM | 0.0568 mL | 0.2840 mL | 0.5680 mL | 1.4199 mL | |
| 60 mM | 0.0473 mL | 0.2366 mL | 0.4733 mL | 1.1832 mL | |
| 80 mM | 0.0355 mL | 0.1775 mL | 0.3550 mL | 0.8874 mL | |
| 100 mM | 0.0284 mL | 0.1420 mL | 0.2840 mL | 0.7099 mL |