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S6 kinase inhibitor
Cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC50‘s at 100µM ATP: RSK1 = 31nM, RSK2 = 24nM, RSK3 = 18nM, RSK4 = 15nM). Does not significantly inhibit 10 other AGC kinases, and over 40 other protein kinases at 100X concentrations. Acts on the N-terminal AGC kinase domain. Completely prevents PMA-induced TSC2 phosphorylation.
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Product Details
| Alternative Name |
2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone |
|---|---|
| Appearance |
Off-white solid. |
| CAS |
501437-28-1 |
| Couple Target |
S6 kinase |
| Couple Type |
Inhibitor |
| Formula |
C19H23F2N5O2 |
| MW |
391.4 |
| Purity |
≥98% (HPLC) |
| Solubility |
Soluble in DMSO (>25mg/ml). |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least one year from the date of receipt when stored as supplied at -20°C |
|---|---|
| Handling |
Solutions can be stored at -20°C for up to 3 months. Protect from moisture and light. |
| Long Term Storage |
-20°C |
| Shipping |
Blue Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Ribosomal S6 kinase signaling regulates neuronal viability during development and confers resistance to excitotoxic cell death in mature neurons: K.R. Hoyt, et al.; Neuroscience 558, 1 (2024), Application(s): Treatment of neuronal cell cultures and stereotactic infusion of mouse brains, Abstract
- Receptor-independent modulation of cAMP-dependent protein kinase and protein phosphatase signaling in cardiac myocytes by oxidizing agents: S. Diering, et al.; J. Biol. Chem. 295, 15342 (2020), Abstract — Full Text
- Low concentrations of cadmium chloride promotes protein translation and improve cell line productivity: Mahameed, M., Obiedat, A., et al.; Biotechnol. Bioeng. 116, 569 (2019), Abstract
- Active Tonic mTORC1 Signals Shape Baseline Translation in Naive T Cells: Myers, D. R., Norlin, E., et al.; Cell Rep. 27, 1858 (2019), Abstract
- EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity: Y. Kaibori, et al.; FASEB J. 33, 5334 (2019), Abstract
- Human melanoma cells resistant to MAPK inhibitors can be effectively targeted by inhibition of the p90 ribosomal S6 kinase: C. Kosnopfel, et al.; Oncotarget 8, 35761 (2017), Application(s): Treatment of patient-derived melanoma cell and other primary cell cultures, Abstract — Full Text
- The Vascular Endothelial Growth Factor-A phosphorylates Murine Double Minute-2 on its Serine 166 via the Extracellular Signal-Regulated Kinase 1/2 and p90 Ribosomal S6 Kinase in primary human endothelial cells: J. Aiken & O. Birot; Biochem. Biophys. Res. Commun. 487, 1548 (2016), Abstract
- Feedback activation of neurofibromin terminates growth factor-induced Ras activation: Hennig, A., Markwart, R., et al.; Cell Commun. Signal. 14, 5 (2016), Abstract
- Phospholipase C∈ Activates Nuclear Factor-κB Signaling by Causing Cytoplasmic Localization of Ribosomal S6 Kinase and Facilitating Its Phosphorylation of Inhibitor κB in Colon Epithelial Cells: M. Wakita, et al.; J. Biol. Chem. 291, 12586 (2016), Application(s): Cell culture treatment, Abstract — Full Text
- ERK and RSK are necessary for TRH-induced inhibition of r-ERG potassium currents in rat pituitary GH3 cells: L. Carretero, et al.; Cell. Signal. 27, 1720 (2015), Application(s): Cell Culture, Abstract
- Simultaneous targeting of PI3Kδ and a PI3Kδ-dependent MEK1/2-Erk1/2 pathway for therapy in pediatric B-cell acute lymphoblastic leukemia: Wang, X., Zhang, X., et al.; Oncotarget 5, 10732 (2014), Abstract
- Modelling negative feedback networks for activating transcription factor 3 predicts a dominant role for miRNAs in immediate early gene regulation: Tindall, M. J., Clerk, A., et al.; PLoS Comput. Biol. 10, e1003597 (2014), Abstract
- Ribosomal S6 kinase regulates ischemia-induced progenitor cell proliferation in the adult mouse hippocampus: K. Karelina, et al.; Exp. Neurol. 253, 72 (2014), Application(s): Stereotactic injection in mice and treatment of primary mouse neurosphere cultures , Abstract — Full Text
- Phosphorylation of KIBRA by the extracellular signal-regulated kinase (ERK)–ribosomal S6 kinase (RSK) cascade modulates cell proliferation and migration: S. Yang, et al.; Cell. Signal. 26, 343 (2014), Application(s): Treatment of MCF-7 cell cultures, Abstract — Full Text
- p90 Ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to Gq-protein-coupled receptor stimuli, endothelin-1 and α1-adrenergic receptor agonists: E. Amirak, et al.; Biochem. J. 450, 351 (2013), Application(s): Rat cadiomyocyte treatment, Abstract — Full Text
- Synthetic Lethality Screen Identifies RPS6KA2 as Modifier of Epidermal Growth Factor Receptor Activity in Pancreatic Cancer: N. Milosevic, et al.; Neoplasia 15, 1354 (2013), Application(s): Cell culture treatment, Abstract — Full Text
- The p90 Ribosomal S6 Kinase (RSK) Is a Mediator of Smooth Muscle Contractility: M. Artamonov, et al.; PLoS One 8, e58703 (2013), Application(s): Treatment of rabbit pulmonary artery tissue, muscle tissue, and mouse ileum tissue cultures, Abstract — Full Text
- Phosphorylation of serine 4,642 in the C-terminus of plectin by MNK2 and PKA modulates its interaction with intermediate filaments: Bouameur, J. E., Schneider, Y., et al.; J. Cell Sci. 126, 4195 (2013), Abstract
- BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo: G. Sapkota, et al.; Biochem. J. 401, 29 (2007), Abstract — Full Text
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