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SB-747651A Dihydrochloride

Catalog No. T9652 CAS 1781882-72-1

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

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SB-747651A Dihydrochloride Chemical Structure

SB-747651A Dihydrochloride, CAS 1781882-72-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 113.00
5 mg	In stock	$ 262.00
10 mg	In stock	$ 386.00
25 mg	In stock	$ 647.00
50 mg	In stock	$ 922.00
100 mg	In stock	$ 1,250.00
500 mg	In stock	$ 2,490.00
1 mL * 10 mM (in DMSO)	In stock	$ 287.00

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Purity: 97.02%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].
In vitro	SB-747651A dihydrochloride (5 μM; neutrophils) modulates neutrophil behavior in response to the CXCL2 chemotactic gradient in various ways. It influences CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner, obstructing the movement of adherent neutrophils to optimal emigration sites. Furthermore, it notably prolongs the transmigration and detachment times of neutrophils, indicating a significant impact on the mechanisms overseeing their transendothelial migration. Additionally, while SB-747651A dihydrochloride slows the migration velocity of extravascular chemotaxing neutrophils, it does not alter their directionality towards CXCL2 signals.
In vivo	SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride has been shown to significantly increase neutrophil adhesion between 3.5 and 4.5 hours after stimulation with CXCL2, in comparison to the effect solely attributable to CXCL2 [3]. Additionally, the same compound administered intraperitoneally (i.p.) at the same dosage enhanced neutrophil extravasation, specifically by augmenting neutrophil emigration at the 3 and 4-hour marks within a mouse peritonitis model for acute inflammation [3]. The experiments were conducted using male C57BL/6N mice aged between 8 to 16 weeks, establishing that a 3 mg/kg dosage, when given as an intrascrotal injection, effectively results in heightened neutrophil adhesion subsequent to CXCL2 stimulation.

Molecular Weight	415.32
Formula	C16H24Cl2N8O
CAS No.	1781882-72-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (120.39 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Immunology/Inflammation Compound Library Cytoskeletal Signaling Pathway Compound Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library

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Keywords

SB-747651A Dihydrochloride 1781882-72-1 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK SB747651A Dihydrochloride SB 747651A Dihydrochloride SB-747651A inhibitor inhibit

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