Name: BI-D1870
Price: 320.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    BI-D1870 is a cell-permeable inhibitor of the p90 RSK isoforms with IC50 values of 31nM, 24nM, 18nM and 15nM for RSK1, RSK2, RSK3 and RSK4 respectively [1].
    BI-D1870 is a derivative of dihydropteridinone and found to be a remarkably specific inhibitor of RSK isoforms. It is an ATP-competitive inhibitor. When the concentrations of ATP are 10μM and 100μM, the IC50 values of BI-D1870 against RSK1 and RSK2 are 5nM, 10nM and 10nM, 20nM, respectively. BI-D1870 also inhibits RSK3 and RSK4 with IC50 values of 18nM and 15nM respectively, when ATP is 100μM. 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 [1].
    
    [1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38.
- Properties
  - Alternative Name
    
    2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
    
    CAS Number
    
    501437-28-1
    
    Molecular Formula
    
    C19H23F2N5O2
    
    Molecular Weight
    
    391.42
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥19.55 mg/mL in DMSO; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Sechi M, Lall RK, et al. "Fisetin targets YB-1/RSK axis independent of its effect on ERK signaling:insights from in vitro and in vivo melanoma models." Sci Rep. 2018 Oct 24;8(1):15726. PMID:30356079

BI-D1870

BI-D1870

Background

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