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1781882-72-1

1781882-72-1 structure
1781882-72-1 structure
  • Name: SB 747651A dihydrochloride
  • Chemical Name: N-{[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl]methyl}-4-piperidinamine dihydrochloride
  • CAS Number: 1781882-72-1
  • Molecular Formula: C16H24Cl2N8O
  • Molecular Weight: 415.32
  • Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
  • Create Date: 2021-01-07 11:22:41
  • Modify Date: 2024-01-03 10:46:16
  • SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research[1].
Name N-{[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl]methyl}-4-piperidinamine dihydrochloride
Synonyms 1H-Imidazo[4,5-c]pyridine-7-methanamine, 2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-, hydrochloride (1:2)
N-{[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl]methyl}-4-piperidinamine dihydrochloride
Description SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research[1].
Related Catalog
Target

IC50: 11 nM (MSK1)[1]
In Vitro SB-747651A dihydrochloride (5 μM; neutrophils) affects CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner. SB-747651A dihydrochloride thwarts the intraluminal crawling of adherent neutrophils to optimal sites of emigration. SB-747651A dihydrochloride (5 μM; neutrophils) significantly increases transmigration time and detachment time. SB-747651A dihydrochloride affects mechanisms that regulate transendothelial migration of neutrophils in response to CXCL2 chemotactic gradient. SB-747651A dihydrochloride inhibits the migration speed of extravascular chemotaxing neutrophils but does not affect their directionality in response to CXCL2 chemotactic gradient[2].
In Vivo SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride 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.) dihydrochloride 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)[3] 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.
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.

[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.
Molecular Formula C16H24Cl2N8O
Molecular Weight 415.32
Exact Mass 414.145020

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title: CAS No. 1781882-72-1 | Chemsrc address: https://m.chemsrc.com/en/baike/1567525.html

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