SB-747651A

SB-747651A is a specific mitogen- and stress-activated kinase 1 (MSK1) inhibitor. SB-747651A can be used for the research of inflammation[1].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

MSK1[1]

SB-747651A (5 μM; neutrophils) affects CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner. SB-747651A thwarts the intraluminal crawling of adherent neutrophils to optimal sites of emigration. SB-747651A (5 μM; neutrophils) significantly increases transmigration time and detachment time. SB-747651A affects mechanisms that regulate transendothelial migration of neutrophils in response to CXCL2 chemotactic gradient. SB-747651A inhibits the migration speed of extravascular chemotaxing neutrophils but does not affect their directionality in response to CXCL2 chemotactic gradient[1].

SB747651A (3 mg/kg; intrascrotal injection) results in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2[1]. SB-747651A (3 mg/kg; i.p.) affects neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation[1]. Animal Model: Male C57BL/6N mice (8~16 weeks)[1] Dosage: 3 mg/kg Administration: Intrascrotal injection Result: Resulted in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2. Animal Model: Male C57BL/6N mice (8~16 weeks)[1] Dosage: 3 mg/kg Administration: I.p. Result: Affected neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation.

[1]. Feiner B, et al. Risperidone effects on heterochromatin: the role of kinase signaling. Clin Exp Immunol. 2019;196(1):67-75.

[2]. Hossain M, et al. The Specific Mitogen- and Stress-Activated Protein Kinase MSK1 Inhibitor SB-747651A Modulates Chemokine-Induced Neutrophil Recruitment. Int J Mol Sci. 2017;18(10):2163. Published 2017 Oct 17.