1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. 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 (24):

Cat. No. Product Name Effect Purity
  • HY-12866A
    Larotrectinib sulfate Inhibitor 99.10%
    Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
  • 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
    Larotrectinib Inhibitor 98.92%
    Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
  • HY-16961
    Sitravatinib Inhibitor 99.85%
    Sitravatinib (MGCD516; MG516) is an orally bioavailable, receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT , FLT3, DDR2, DDR1, TRKA, TRKB, respectively.
  • 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-50867
    Lestaurtinib Inhibitor >99.0%
    Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  • HY-W013372
    7,8-Dihydroxyflavone Agonist 99.74%
    7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases.
  • HY-112434
    Trk-IN-3 Inhibitor
    Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
  • HY-12497
    ANA-12 Antagonist 99.95%
    ANA-12 is a potent and selective TrkB antagonist with IC50s of 45.6 nM and 41.1 μM for the high and low affinity sites, respectively.
  • HY-18314
    GW 441756 Inhibitor 99.32%
    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-103022
    Repotrectinib Inhibitor 99.91%
    Repotrectinib (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-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-13491
    GNF-5837 Inhibitor 98.44%
    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-101977
    Selitrectinib Inhibitor 99.90%
    Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor (TKI), with IC50s of 0.6 nM, <2.5 nM for TRKA and TRKC respectively.
  • HY-100673
    LM22A-4 Agonist >98.0%
    LM22A-4 is a specific agonist of tyrosine kinase receptor B, used for neurological disease research.
  • HY-17622
    Tavilermide Agonist >98.0%
    Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
  • 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-107362
    CH7057288 Inhibitor 98.52%
    CH7057288 is a potent and selective TRK inhibitor.
  • HY-15590
    AZ-23 Inhibitor 99.93%
    AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C 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.
Isoform Specific Products

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