2. Signaling Pathways
  3. Neuronal Signaling
    Protein Tyrosine Kinase/RTK
  4. Trk Receptor

Trk Receptor

Tropomyosin related kinase receptor

Trk Receptor

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Trk receptors are a family of three receptor tyrosine kinases (TrkA, TrkB, and TrkC), each of which can be activated by one or more of four neurotrophins-nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), and neurotrophins 3 and 4 (NT3 and NT4).

TrkA, TrkB, and TrkC are transmembrane proteins that comprise the TRK receptor family. These receptor tyrosine kinases are expressed in human neuronal tissue, and play an essential role in both the physiology of development and function of the nervous system through activation by neurotrophins (NTs). The latter are specific ligands known as NGF for TrkA, BDGF, and NT-4/5 for TrkB and NT3 for TrkC, respectively.

The binding of the ligand to the receptor triggers the oligomerisation of the receptors and phosphorylation of specific tyrosine residues in the intracytoplasmic kinase domain. This event results into the activation of signal transduction pathways leading to proliferation, differentiation and survival in normal and neoplastic neuronal cells.

Trk Receptor Isoform Specific Products:

Trk Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12678
    Entrectinib
    		Inhibitor 99.87%
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib
  • HY-12866
    Larotrectinib
    		Inhibitor 99.95%
    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).
    Larotrectinib
  • HY-12497
    ANA-12
    		Antagonist 99.91%
    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.
    ANA-12
  • HY-W013372
    7,8-Dihydroxyflavone
    		Agonist 99.90%
    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.
    7,8-Dihydroxyflavone
  • HY-103022
    Repotrectinib
    		Inhibitor 99.90%
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
    Repotrectinib
  • HY-121833
    Gambogic amide
    		Agonist ≥98.0%
    Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke.
    Gambogic amide
  • HY-12678S
    Entrectinib-d4
    		Inhibitor
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib-d<sub>4</sub>
  • HY-137465
    CG428
    		Degrader
    CG428 is a potent and selective tropomyosin receptor kinase (TRK) degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells (DC50 = 0.36 nM) and inhibits downstream PLCγ1phosphorylation (IC50 = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC50 = 2.9 nM).
    CG428
  • HY-16961
    Sitravatinib
    		Inhibitor 99.59%
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3/Flt-4, VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
    Sitravatinib
  • HY-B0527A
    Amitriptyline hydrochloride
    		Agonist 98.91%
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
    Amitriptyline hydrochloride
  • HY-18314
    GW 441756
    		Inhibitor 99.95%
    GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth.
    GW 441756
  • HY-13491
    GNF-5837
    		Inhibitor 99.65%
    GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
    GNF-5837
  • HY-107854
    N-Acetyl-5-hydroxytryptamine
    		Activator 99.96%
    N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor.
    N-Acetyl-5-hydroxytryptamine
  • HY-50867
    Lestaurtinib
    		Inhibitor 99.17%
    Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor.
    Lestaurtinib
  • HY-101977
    Selitrectinib
    		Inhibitor 99.90%
    Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.
    Selitrectinib
  • HY-104047
    LM22B-10
    		Activator 99.92%
    LM22B-10 is an activator of TrkB/TrkC neurotrophin receptor, and can induce TrkB, TrkC, AKT and ERK activation in vitro and in vivo.
    LM22B-10
  • HY-12866A
    Larotrectinib sulfate
    		Inhibitor 98.96%
    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).
    Larotrectinib sulfate
  • HY-B0791
    Altiratinib
    		Inhibitor 98.05%
    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/KDR/Flk-1, FLT3, Trk1, Trk2, and Trk3 respectively.
    Altiratinib
  • HY-15590
    AZ-23
    		Inhibitor 98.57%
    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.
    AZ-23
  • HY-P1178
    Cyclotraxin B
    		Inhibitor 98.01%
    Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
    Cyclotraxin B
Cat. No. Product Name / Synonyms Application Reactivity
Trk Receptor Isoform Comparison

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