SB 747651A dihydrochloride

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Cat.No. 4630 - SB 747651A dihydrochloride | C16H22N8O.2HCl | CAS No. 1781882-72-1
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)
Datasheet
Citations (1)
Reviews
Literature

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.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Compound Libraries

SB 747651A dihydrochloride is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox II and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 415.32
Formula C16H22N8O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1781882-72-1
PubChem ID 90488958
InChI Key NRRCQHARLPNLHJ-UHFFFAOYSA-N
Smiles NC1=NON=C1C3=NC2=CN=CC(CNC4CCNCC4)=C2N3CC.Cl.Cl

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.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 415.32. Batch specific molecular weights may vary from batch to batch due to solvent 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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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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

1 Citation for SB 747651A dihydrochloride

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


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