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Cat. No. M1948
BI-D1870 Structure
Size Price Availability Quantity
5mg USD 133  USD133 In stock
10mg USD 215  USD215 In stock
50mg USD 580  USD580 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • 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).

Customer Product Validations & Biological Datas
Source Cell Death Dis (2013). Figure 5. BI-D1870
Method FACS analyses
Cell Lines HCT116 cells
Concentrations 10 μM
Incubation Time 24 h
Results BI-D1870 by itself induced massive apoptosis in p21-deficient cells, whereas wild-type and p53-/- cells were killed by this compound to a much lesser extent, suggesting a close functional relationship between RSKs and p21.
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
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 391.42
Formula C19H23F2N5O2
CAS Number 501437-28-1
Purity >98%
Solubility DMSO 68 mg/mL
Storage at -20°C

[1] Sapkota GP, et al. Biochem J. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo.

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Keywords: BI-D1870 supplier, S6 Kinase, inhibitors

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