SB 747651A dihydrochloride
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%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Effects of hypnotic bromovalerylurea on microglial BV2 cells
S Kawasaki, N Abe, F Ohtake, A Islam, ME Choudhury, R Utsunomiya, S Kikuchi, T Nishihara, J Kuwabara, H Yano, Y Watanabe, M Aibiki, T Yorozuya, J Tanaka
J. Pharmacol. Sci., 2017;0(0):. -
Translational control of PML contributes to TNFalpha-induced apoptosis of MCF7 breast cancer cells and decreased angiogenesis in HUVECs.
Hsu K, Guan B, Cheng X, Guan D, Lam M, Hatzoglou M, Kao H
Cell Death Differ, 2015;23(3):469-83. -
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Bamford et al.
Bioorg.Med.Chem.Lett., 2005;15:3402 -
(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.
Bamford et al.
Bioorg.Med.Chem.Lett., 2005;15:3407 -
Characterization of the cellular action of the MSK inhibitor SB-747651A.
Naqvi et al.
Biochem.J., 2012;441:347
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Citations for SB 747651A dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for SB 747651A dihydrochloride include:
8 Citations: Showing 1 - 8
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Growth State-Dependent Activation of eNOS in Response to DHA: Involvement of p38 MAPK.
Authors: Carla G Et al.
Int J Mol Sci 2023;24
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MEK inhibitor resistance in lung adenocarcinoma is associated with addiction to sustained ERK suppression.
Authors: Marc Et al.
NPJ Precis Oncol 2022;6:88
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Dual targeting of brain region-specific kinases potentiates neurological rescue in Spinocerebellar ataxia type 1.
Authors: Juan Et al.
EMBO J 2021;40:e106106
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Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer.
Authors: Marc Et al.
Elife 2021;10
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MicroRNA-130a Contributes to Type-2 Classical DC-activation in Sj�gren's Syndrome by Targeting Mitogen- and Stress-Activated Protein Kinase-1.
Authors: Lopes Et al.
Front Immunol 2019;10:1335
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Reduction of protein kinase A-mediated phosphorylation of ATXN1-S776 in Purkinje cells delays onset of Ataxia in a SCA1 mouse model.
Authors: Nissa Et al.
Neurobiol Dis 2018;116:93-105
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Inflammatory but not mitogenic contexts prime synovial fibroblasts for compensatory signaling responses to p38 inhibition.
Authors: Jones Et al.
Sci Signal 2018;11
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The mitogen and stress-activated protein kinase 1 regulates the rapid epigenetic tagging of dorsal horn neurons and nocifensive behaviour.
Authors: Tochiki Et al.
Pain 2016;157:2594
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IL10 inhibition
In vitro, inhibition of IL10
In vitro study of MSK1 in pancreatic cancer
