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Trk Receptors

Trk receptor inhibitors act on tropomyosin receptor kinases (Trk), the receptor tyrosine kinases for neurotrophins. Tropomyosin receptor kinases A, B and C (TrkA, TrkB, TrkC) are encoded by the neurotrophic receptor tyrosine kinase genes (NTRK1, NTRK2, NTRK3). In 1991 TrkA was identified as a signal-transducing receptor for nerve growth factor (NGF). In the same year TrkB was shown to bind brain-derived neurotrophic factor (BDNF) and neurotrophin-3. The receptors support neuronal survival and synaptic plasticity, and NTRK1-3 gene fusions are studied in several tumor types. Entrectinib inhibits all three Trk receptors together with c-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK). AZ 23 targets TrkA and TrkB, whereas ANA-12 is a TrkB inhibitor used to probe BDNF signaling.

1 Item

  • CG428
    Cat. No.
    A34980
    CAS No.
    2412055-93-5

    CG428

    CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma.

    In stock View Details
    1 mg
    $140.00
    5 mg
    $365.00
    All 7 sizes

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