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.
Product Details
| Alternative Name: | 2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone |
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| Formula: | C19H23F2N5O2 |
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| MW: | 391.4 |
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| CAS: | 501437-28-1 |
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| Purity: | ≥98% (HPLC) |
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| Appearance: | Off-white solid. |
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| Solubility: | Soluble in DMSO (>25mg/ml). |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stable for at least one year from the date of receipt when stored as supplied at -20°C |
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| Handling: | Solutions can be stored at -20°C for up to 3 months. Protect from moisture and light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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
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;
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;
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
