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)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
DMSO
20.77
50
water
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
1 mM
2.41 mL
12.04 mL
24.08 mL
5 mM
0.48 mL
2.41 mL
4.82 mL
10 mM
0.24 mL
1.2 mL
2.41 mL
50 mM
0.05 mL
0.24 mL
0.48 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Bamfordet 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
Bamfordet 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
Naqviet al (2012) Characterization of the cellular action of the MSK inhibitor SB-747651A. Biochem.J. 441 347 PMID: 21970321