An allosteric antagonist of CXCR1 and CXCR2 (IC50s = 43 and 0.97 nM

SCH 527123 – 10 mg

Brand:
Cayman
CAS:
473727-83-2
Storage:
-20
UN-No:
Non-Hazardous - /

SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

 

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Description

An allosteric antagonist of CXCR1 and CXCR2 (IC50s = 43 and 0.97 nM, respectively); inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human PMNs at 3 nM; inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in BALF in a rat model of airway inflammation; inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively); reduces tumor growth in an HCT116 mouse xenograft model at 50 mg/kg per day

Formal name: 2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-benzamide

Synonyms:  MK-7123

Molecular weight: 397.4

CAS: 473727-83-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases

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