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BI-D1870

Cat. No. M1948
BI-D1870 Structure
Size Price Availability Quantity
10mg USD 250 In stock
50mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro. BI-D1870 does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Additionally, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB (cAMP-response-element-binding protein).

Protocol
Cell Experiment
Cell lines HEK-293 cells
Preparation method Prior to stimulation, cells were cultured in the absence of serum for 16 h. Inhibitors were dissolved in DMSO at a 1000-fold higher concentration than they were used at. These inhibitors, or the equivalent volume of DMSO as a control, were added to the tissue culture medium 30 min prior to stimulation, unless indi-cated otherwise. The final concentration of DMSO in the culture medium was 0.1% and had no effect on agonist-induced activ-ation or phosphorylation of any of the substrates examined. The cells were stimulated with the indicated agonists and lysed in 1 ml of ice-cold Lysis Buffer, and centrifuged at 16000 g at 4 °C for 5 min. The supernatants were frozen in liquid nitrogen and stored at −80 °C until use. Protein concentrations were determined using the Bradford method with BSA as the standard.
Concentrations 10 μM
Incubation time 4 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 391.42
Formula C19H23F2N5O2
CAS Number 501437-28-1
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.
Sapkota GP, et al. Biochem J. 2007 Jan 1;401(1):29-38. PMID: 17040210.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BI-D1870 supplier, S6 Kinase, inhibitors

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