ChemicalBook CAS DataBase List 607372-46-3

607372-46-3

Name	1H-Imidazo[4,5-c]pyridine-7-methanamine, 2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-
CAS	607372-46-3
Molecular Formula	C16H22N8O
MDL Number	MFCD22580418
Molecular Weight	342.4
MOL File	607372-46-3.mol

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Description

SB-747651A is a potent, ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor (IC50 = 11 nM in an in vitro kinase assay). It targets the N-terminal kinase domain. SB-747651A inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells.

Uses

SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research[1].

in vivo

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^[3].
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^[3].

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)^[3]
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.

References

[1] Shaista Naqvi, et al. Characterization of the cellular action of the MSK inhibitor SB-747651A. Biochem J. 2012 Jan 1;441(1):347-57. DOI:10.1042/BJ20110970
[2] Feiner B, et al. Risperidone effects on heterochromatin: the role of kinase signaling. Clin Exp Immunol. 2019;196(1):67-75. DOI:10.1111/cei.13250
[3] 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. DOI:10.3390/ijms18102163

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