GW441756 hydrochloride

A Potent Inhibitor of TrkA
Cat #: G-191
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 311.8
    Purity: ≥97%
    Formulation Lyophilized powder.
    Effective concentration 2 nM - 2 µM.
    Structure
    Chemical name (3Z)-3-[(1-methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one; hydrochloride.
    Molecular formula C17H14ClN3O.
    CAS No.: 504433-24-3 (free base).
    Activity GW441756 is a potent, selective inhibitor of the NGF receptor tyrosine kinase A (TrkA)1.
    References - Activity
    1. Wood, E.R. et al. (2004) Bioorg. Med. Chem. Lett. 14, 953.

    Storage before reconstitution Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Reconstitution 4-10 mM in H2O. Centrifuge all product preparations before use (5,000 x g for 1 min).
    Storage after reconstitution Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    Alomone Labs GW441756 hydrochloride inhibits NGF-induced survival of PC12 cells. 
    PC12 cells were incubated for 24 hours with or without 2 nM Native mouse NGF 2.5S protein (>95%) (#N-100), inducing 5 fold increase in cell numbers measured with XTT. Increasing concentrations of GW441756 hydrochloride (#G-191), induced dose dependent inhibition of the NGF effect with apparent IC50 of about 2 µM.
    References - Scientific Background
    1. Green, S.H. et al. (2012) Anat. Rec. 295, 1877.
    2. Wood, E.R. et al. (2004) Bioorg. Med. Chem. Lett. 14,953.
    Scientific background

    GW441756 is a potent and selective inhibitor of the NGF receptor tyrosine kinase A (TrkA). This compound also inhibits TrkB and TrkC but displays significantly higher selectivity for TrkA receptor than other TrkA inhibitors and a 100-fold selectivity over a range of other kinases. The IC50 value of GW441756 is 2 nM1,3.

    The compound induces a dose-dependent decrease in neoplastic proliferation and has the ability to increase levels of caspase-3 that can lead to apoptosis.

    Previous studies have shown that TrKA inhibitors have a relevant anti-proliferative effects in neoplasia compare to other TrkA inhibitors with a lower effective dosage1,3.

    Signaling through protein tyrosine kinase receptors is important for neuronal metabolism, promotion of neuronal survival, stimulating neurite growth, synaptogenesis and potentiating synaptic strength2.

    Target TrkA receptors
    Last update: 05/03/2019

    GW441756 hydrochloride (#G-191) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use