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

Trk Receptor

Tropomyosin related kinase receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112423
    CE-245677
    Inhibitor 98.14%
    CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.
    CE-245677
  • HY-151948
    TrkA-IN-3
    Inhibitor 98.46%
    TrkA-IN-3 is a potent, subselective and allosteric TrkA inhibitor, with an IC50 of 22.4 nM. TrkA-IN-3 shows more than 8000-fold selectivity for TrkA over TrkB and TrkC. TrkA-IN-3 can be used for the research of pain.
    TrkA-IN-3
  • HY-129634
    TrkA-IN-1
    Inhibitor
    TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity.
    TrkA-IN-1
  • HY-112437
    PF-06737007
    Inhibitor 99.70%
    PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
    PF-06737007
  • HY-P99200
    Fulranumab
    Inhibitor
    Fulranumab is a human IgG2 monoclonal antibody against nerve growth factor (NGF) and can be used for the research of pain.
    Fulranumab
  • HY-135096
    Amitriptyline-d3 hydrochloride
    Agonist 99.46%
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). 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-d3 hydrochloride
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    Agonist 99.03%
    Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-102066
    Utatrectinib
    Inhibitor 98.72%
    Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.
    Utatrectinib
  • HY-151949
    TrkA-IN-4
    Inhibitor 99.90%
    TrkA-IN-4, a potent, orally active and allosteric TrkA inhibitor, is a proagent of TrkA-IN-3 (IC50=22.4 nM, HY-151948). TrkA-IN-4 exhibits potent antinociceptive effects.
    TrkA-IN-4
  • HY-107854S
    N-Acetyl-5-hydroxytryptamine-d3
    Activator ≥98.0%
    N-Acetyl-5-hydroxytryptamine-d3 is the deuterium labeled N-Acetyl-5-hydroxytryptamine. N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor[1][2].
    N-Acetyl-5-hydroxytryptamine-d<sub>3</sub>
  • 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-157148
    1D228
    Inhibitor
    1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors.
    1D228
  • HY-152472
    ENT-C225
    Activator 99.16%
    ENT-C225 is an effective activator of TrkB neurotrophin receptor. ENT-C225 has high effect on activating TrkB receptor (TrkBR), and has good physicochemical properties and neuroprotective properties.
    ENT-C225
  • HY-16961A
    Sitravatinib malate
    Inhibitor
    Sitravatinib malate (MGCD516 malate) 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 malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
    Sitravatinib malate
  • HY-132229
    LPM4870108
    Inhibitor
    LPM4870108 is a potent and orally active pan-Trk (WT and MT) inhibitor, with IC50s of 0.2 nM, 2.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA, TrkAG595R and TrkAG667C, respectively. LPM4870108 shows selectivity for Trk over ALK (IC50=182 nM). LPM4870108 exhibits anti-tumor activity.
    LPM4870108
  • HY-146749
    FLT3/TrKA-IN-1
    Inhibitor
    FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML).
    FLT3/TrKA-IN-1
  • HY-112434
    PF-06733804
    Inhibitor
    PF-06733804 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.
    PF-06733804
  • HY-147303
    Sacibertinib
    Inhibitor
    Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity.
    Sacibertinib
  • HY-137465
    CG428
    Degrader
    CG428 is a potent and selective tropomyosin receptor kinase (TRK) PROTAC 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).(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))
    CG428
  • HY-146523
    TRK-IN-17
    Inhibitor
    TRK-IN-17 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-17 has the potential for the research of cancer diseases (extracted from patent WO2021148807A1, compound 3).
    TRK-IN-17
Cat. No. Product Name / Synonyms Application Reactivity

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