SB-747651A
Based on 2 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 607372-46-3
- Formula: C16H22N8O
- Molecular Weight:342.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) SB-747651A
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Biological Activity
IC50: 11 nM (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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6N mice (8~16 weeks)[1]
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Dosage:3 mg/kg
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Administration:Intrascrotal injection
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Result:Resulted in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2.
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Animal Model:Male C57BL/6N mice (8~16 weeks)[3]
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Dosage:3 mg/kg
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Administration:I.p.
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Result:Affected neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation.
Chemical Information
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CAS No. 607372-46-3
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Molecular Weight 342.40
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Formula C16H22N8O
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SMILES
NC1=NON=C1C(N2CC)=NC3=C2C(CNC4CCNCC4)=CN=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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J Cell Sci
2025 Sep 16:jcs.264193. PMID: 40955174 -
Purity & Documentation
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. [Content Brief]
[2]. Feiner B, et al. Risperidone effects on heterochromatin: the role of kinase signaling. Clin Exp Immunol. 2019;196(1):67-75. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)