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-110255A
    AZD 2066 hydrate
    Activator ≥99.0%
    AZD-2066 hydrate is a selective, orally active and blood-brain barrier-permeating mGluR5 antagonist. AZD 2066 hydrate activates the BDNF/trkB signaling pathway. AZD 2066 hydrate can be used in the research of neuropathic pain, major depressive disorder and gastroesophageal reflux disease.
    AZD 2066 hydrate
  • 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
  • HY-157168
    TrkA-IN-6
    Inhibitor
    TrkA-IN-6 (compound R48) is a hydrazone-like, selective inhibitor of tropomyosin kinase type A receptor kinase (TrkA). TrkA-IN-6 exhibited a higher cytotoxic effect on U87 GBM cells than Temozolomide (HY-17364), with an IC50 of 68.99 μM.
    TrkA-IN-6
  • HY-156086
    TRK-IN-24
    Inhibitor
    TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKAG595R, TRKAG667C and TRKAF589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1G595R and BaF3-CD74-NTRK1G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM.
    TRK-IN-24
  • HY-P10529
    Ganglioside GM1-binding peptides p3
    Inhibitor
    Ganglioside GM1-binding peptides p3 is a synthetic peptide that can specifically bind to the pentasaccharide part of GM1 ganglioside. The dynamic transformation of Ganglioside GM1-binding peptides p3 may play an important role in the function of GM1 as a multiple receptor, such as in the classical pathway of cholera toxin infection. Ganglioside GM1-binding peptides p3 can be used to study the interaction between GM1 and its ligands.
    Ganglioside GM1-binding peptides p3
  • HY-123237
    KRC-108
    Inhibitor
    KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice.
    KRC-108
  • HY-161819
    TRK-IN-29
    Inhibitor
    TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKAG595R, TRKAF589L, TRKAG667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties.
    TRK-IN-29
  • HY-143557
    Trk-IN-7
    Inhibitor
    Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50=5-50 nM).
    Trk-IN-7
  • HY-145105
    Inonophenol C
    Inonophenol C is a neurotrophic and protective agent against neurodegenerative disorders.
    Inonophenol C
  • HY-146115
    TRK-IN-19
    Inhibitor
    TRK-IN-19 (Compound I-10 ) is a potent inhibitor of TRK (TRKA IC50 = 1.1 nM, TRKAG595R IC50 = 5.3 nM). TRK-IN-19 has the potential for the research of cancer diseases.
    TRK-IN-19
Cat. No. Product Name / Synonyms Application Reactivity

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