SB 747651A dihydrochloride
Chemical Name: 2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-N-4-piperidinyl-1H-imidazo[4,5-c]pyridine-7-methanamine dihydrochloride
Purity: ≥98%
Biological Activity
Potent, ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor (IC50 = 11 nM in an in vitro kinase assay); targets the N-terminal kinase domain. Inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. Blocks IL-10 production in macrophages.Technical Data
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Background References
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(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Bamford et al.
Bioorg.Med.Chem.Lett., 2005;15:3402 -
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors.
Bamford et al.
Bioorg.Med.Chem.Lett., 2005;15:3407 -
Characterization of the cellular action of the MSK inhibitor SB-747651A.
Naqvi et al.
Biochem.J., 2012;441:347
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Citation for SB 747651A dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for SB 747651A dihydrochloride include:
1 Citation: Showing 1 - 1
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The mitogen and stress-activated protein kinase 1 regulates the rapid epigenetic tagging of dorsal horn neurons and nocifensive behaviour.
Authors: Tochiki Et al.
Pain 2016;157:2594
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