BX795

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    BX795, a small molecule with an aminopyrimidine backbone in its chemical structure, is a potent and ATP-competitive inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) that binds to the ATP binding pocket of PDK1 and hence potently inhibits the enzymatic activity of PDK1 in a direct kinase assay format with a value of 50% concentration inhibition IC50 of 11 nM. BX795 is also a potent and selectively inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase ε (IKKε), with values of IC50 of 0.006 μM and 0.041 μM respectively, that blocks the phosphorylation, nuclear translocation and transcriptional activity of interferon regulatory factor 3 as well as the production of interferon-β in macrophages stimulated with poly(I:C) or lipopolysaccharide (LPS).
- Properties
  - Alternative Name
    
    N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
    
    CAS Number
    
    702675-74-9
    
    Molecular Formula
    
    C23H26IN7O2S
    
    Molecular Weight
    
    591.48
    
    Appearance
    
    A solid
    
    Purity
    
    98.13%
    
    Solubility
    
    ≥59.1 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Mlcochova P, Winstone H, et al. "TLR4-Mediated Pathway Triggers Interferon-Independent G0 Arrest and Antiviral SAMHD1 Activity in Macrophages." Cell Rep. 2020;30(12):3972-3980.e5. PMID:32209460

BX795

Background

We Also Recommend

CID 2011756

Ezatiostat

StemRegenin 1 (SR1)