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BI-D1870

S6 kinase inhibitor
 
BML-EI407-0001 1 mg 74.00 USD
 
BML-EI407-0005 5 mg 214.00 USD
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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 Specification

Alternative Name:2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone
 
Formula:C19H23F2N5O2
 
MW:391.4
 
CAS:501437-28-1
 
Purity:≥98% (HPLC)
 
Appearance:Off-white solid.
 
Solubility:Soluble in DMSO (>25mg/ml).
 
Shipping:Shipped on Blue Ice
 
Long Term Storage:-20°C
 
Use/Stability: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.
 
Regulatory Status:RUO - Research Use Only
 
BML-EI407 structure
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BML-EI407 structure

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. (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

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