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SB 747651A dihydrochloride is a 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.
Sold with the permission of GlaxoSmithKline.
SB 747651A dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 415.32. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.82 mL||24.08 mL||48.16 mL|
|2.5 mM||0.96 mL||4.82 mL||9.63 mL|
|5 mM||0.48 mL||2.41 mL||4.82 mL|
|25 mM||0.1 mL||0.48 mL||0.96 mL|
References are publications that support the biological activity of the product.
Bamford et al (2005) (1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors. Bioorg.Med.Chem.Lett. 15 3402 PMID: 15950465
Bamford et al (2005) (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. Bioorg.Med.Chem.Lett. 15 3407 PMID: 15955699
Naqvi et al (2012) Characterization of the cellular action of the MSK inhibitor SB-747651A. Biochem.J. 441 347 PMID: 21970321
If you know of a relevant reference for SB 747651A dihydrochloride, please let us know.
Keywords: SB 747651A dihydrochloride, SB 747651A dihydrochloride supplier, SB747651A, mitogen, and, stress, activated, kinase, inhibitors, inhibits, MSK1, MSK2, potent, IL-10, production, cell, permeable, AGC, group, Other, Kinases, 4630, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for SB 747651A dihydrochloride include:
Tochiki et al (2016) The mitogen and stress-activated protein kinase 1 regulates the rapid epigenetic tagging of dorsal horn neurons and nocifensive behaviour. Pain 157 2594 PMID: 27482631
Lopes et al (2019) MicroRNA-130a Contributes to Type-2 Classical DC-activation in Sjögren's Syndrome by Targeting Mitogen- and Stress-Activated Protein Kinase-1. Front Immunol 10 1335 PMID: 31281310
Jones et al (2018) Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition. Sci Signal 11 PMID: 29511118
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