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Submit ReviewSB 747651A dihydrochloride
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 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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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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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
8 Citations for SB 747651A dihydrochloride
Citations are publications that use Tocris products. Selected citations for SB 747651A dihydrochloride include:
Jones et al (2018) Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition. Sci Signal 11 PMID: 29511118
Marc et al (2021) Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. Elife 10 PMID: 34121659
Juan et al (2021) Dual targeting of brain region-specific kinases potentiates neurological rescue in Spinocerebellar ataxia type 1. EMBO J 40 e106106 PMID: 33709453
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
Nissa et al (2018) Reduction of protein kinase A-mediated phosphorylation of ATXN1-S776 in Purkinje cells delays onset of Ataxia in a SCA1 mouse model. Neurobiol Dis 116 93-105 PMID: 29758256
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
Marc et al (2022) MEK inhibitor resistance in lung adenocarcinoma is associated with addiction to sustained ERK suppression. NPJ Precis Oncol 6 88 PMID: 36418460
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
Do you know of a great paper that uses SB 747651A dihydrochloride from Tocris? Please let us know.
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