1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor

Trk Receptor

TrkA (TRK1-transforming tyrosine kinase protein) is a protein that in humans is encoded by the NTRK1 gene. TrkA is a member of the neurotrophic tyrosine kinase receptor (NTKR) family. TrkA is a membrane-bound receptor that, upon neurotrophin binding, phosphorylates itself (autophosphorylation) and members of the MAPK pathway. TrkA is the high affinity catalytic receptor for the neurotrophin, Nerve Growth Factor, which include neuronal differentiation and avoidance of programmed cell death. The presence of TrkA leads to cell differentiation and may play a role in specifying sensory neuron subtypes. Mutations in TrkA gene have been associated with congenital insensitivity to pain with anhidrosis, self-mutilating behavior, mental retardation and cancer.

TrkB has the highest affinity to the binding of brain-derived neurotrophic factor (BDNF) and NT-4. BDNF is a growth factor that has important roles in the survival and function of neurons in the central nervous system. The binding of BDNF to TrkB receptor causes many intercellular cascades to be activated, which regulate neuronal development and plasticity, long-term potentiation, and apoptosis.

TrkC is ordinarily activated by binding with NT-3 and has little activation by other ligands. (TrkA and TrkB also bind NT-3, but to a lesser extent). TrkC is mostly expressed by proprioceptive sensory neurons.

Trk Receptor Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-12678
    Entrectinib Inhibitor 99.61%
    Entrectinib is a potent and orally available Trk, ROS1, and ALK inhibitor; inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively.
  • HY-12866
    LOXO-101 Inhibitor 98.92%
    LOXO-101 is a potent, ATP competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
  • HY-12497
    ANA-12 Antagonist 99.30%
    ANA-12 is a potent and selective TrkB antagonist, and binds to TrkBECD-Fc with Kd of 12 μM.
  • HY-12866A
    LOXO-101 sulfate Inhibitor 99.21%
    LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
  • HY-104047
    LM22B-10 Activator 98.81%
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
  • HY-101977
    LOXO-195 Inhibitor 98.89%
    LOXO-195 is a next-generation TRK kinase (TKI) inhibitor, with IC50s of 0.6±0.1 nM, <2.5 nM for TRKA and TRKC respectively.
  • HY-107362
    CH7057288 Inhibitor
    CH7057288 is a potent and selective TRK inhibitor.
  • HY-112423
    CE-245677 Inhibitor
    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
  • HY-103022
    TPX-0005 Inhibitor 99.91%
    TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
  • HY-13491
    GNF-5837 Inhibitor 99.01%
    GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).
  • HY-18314
    GW 441756 Inhibitor 98.90%
    GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.
  • HY-100673
    LM22A-4 Agonist >98.0%
    LM22A-4 is a specific agonist of tyrosine kinase receptor B, used for neurological disease research.
  • HY-B0791
    Altiratinib Inhibitor
    Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
  • HY-17603
    Belizatinib Inhibitor 99.32%
    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
  • HY-20878
    Tyrphostin AG 879 Inhibitor 99.10%
    TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.
  • HY-17622
    Tavilermide Agonist >98.0%
    Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
  • HY-15590
    AZ-23 Inhibitor
    AZ-23 is a potent, orally bioavailable Trk kinase inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
  • HY-107854
    N-Acetyl-5-hydroxytryptamine Activator
    N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor.
Isoform Specific Products

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