1. MAPK/ERK Pathway
  2. p38 MAPK
  3. SB-747651A

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (SB-747651A dihydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

SB-747651A Chemical Structure

SB-747651A Chemical Structure

CAS No. : 607372-46-3

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Description

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].

IC50 & Target

IC50: 11 nM (MSK1)[1]

In Vitro

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

342.40

Formula

C16H22N8O

CAS No.
SMILES

NC1=NON=C1C(N2CC)=NC3=C2C(CNC4CCNCC4)=CN=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SB-747651A Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SB-747651A
Cat. No.:
HY-114038
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