product name BI-D1870
Description: BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM in cell-free assays, respectively; it exhibits10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B. The inhibition activity of BI-D1870 against RSK is more than 500-fold greater than some other AGC kinases suggesting BI-D1870 as a specific inhibitor of RSK. In addition, BI-D1870 is reported to induce the phosphorylation of ERK1/ERK2 and the subsequent phosphorylation of CREB in Rat-2 cells.
References: Biochem J. 2007 Jan 1; 401(Pt 1): 29–38.
391.42
Formula
C19H23F2N5O2
CAS No.
501437-28-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 78 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: BI-D1870 inhibits RSK1, RSK2, RSK3 and RSK4 with an IC50 of 10–30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in human embry-onic kidney 293 cells and Rat-2 cells. BI-D1870 does not affect the agonist-triggered phosphorylation of substrates for six other AGC kinases. Moreover, BI-D1870 does not suppress the phorbol ester- or EGF-induced phosphorylation of CREB. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Biochem J. 2007 Jan 1; 401(Pt 1): 29–38. |
