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Submit ReviewSB 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.
Sold with the permission of GlaxoSmithKline.
SB 747651A dihydrochloride is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 415.32 |
公式 | C16H22N8O.2HCl |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 20.77 | 50 | |
DMSO | 20.77 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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
引用文献是使用了 Tocris 产品的出版物。 SB 747651A dihydrochloride 的部分引用包括:
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
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