SB 747651A dihydrochloride

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Description: Potent MSK1 inhibitor; also inhibits other AGC group kinases
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% (HPLC)
Citations (8)

Biological Activity for SB 747651A dihydrochloride

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.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Compound Libraries for SB 747651A dihydrochloride

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.

Technical Data for SB 747651A dihydrochloride

M. Wt 415.32
Formula C16H22N8O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1781882-72-1
PubChem ID 90488958

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.

Solubility Data for SB 747651A dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
water 20.77 50
DMSO 20.77 50

Preparing Stock Solutions for SB 747651A dihydrochloride

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for SB 747651A dihydrochloride

Certificate of Analysis / Product Datasheet
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References for SB 747651A dihydrochloride

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.

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8 Citations for SB 747651A dihydrochloride

Citations are publications that use Tocris products. Selected citations for SB 747651A dihydrochloride include:

Carla G et al (2023) Growth State-Dependent Activation of eNOS in Response to DHA: Involvement of p38 MAPK. Int J Mol Sci 24 PMID: 37176054

Jones et al (2018) Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition. Sci Signal 11 PMID: 29511118

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

Marc et al (2021) Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. Elife 10 PMID: 34121659

Do you know of a great paper that uses SB 747651A dihydrochloride from Tocris? Please let us know.

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