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

Trk Receptor

Tropomyosin related kinase receptor

Trk Receptor

Related Products

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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-P990749
    Luvagrobart
    		Inhibitor 98.80%
    Luvagrobart is an anti-NGF human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
    Luvagrobart
  • HY-149912
    CZS-241
    		Inhibitor
    CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.
    CZS-241
  • HY-117517
    NG-012
    		Activator
    NG-012, potentiator of nerve growth factor (NGF), were isolated from the culture broth of Penicillium verruculosum F-4542. NG-012 potentiates the neurite outgrowth induced by NGF in rat pheochromocytoma cell line (PC12).
    NG-012
  • 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-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-12678R
    Entrectinib (Standard)
    		Inhibitor
    Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. 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 (Standard)
  • 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, VEGFR2, VEGFR1, 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-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-168858
    TRK-IN-30
    		Inhibitor
    TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKAG595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12.
    TRK-IN-30
  • 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-P992345
    DS002
    		Inhibitor
    DS002 is a human monoclonal antibody targeting NGF/bNGF, with an IC50 of 6.60 nM against human NGF, 1.98 nM against rat NGF, and 8.46 nM against mouse NGF. DS002 blocks NGF-TrkA binding, interrupts pain signal transduction, inhibits TrkA-mediated downstream signaling pathways, and alters aromatic amino acid metabolic pathways. DS002 inhibits cancer cell proliferation. DS002 exerts a preventive effect on Paclitaxel-, Cisplatin- and Vincristine-induced peripheral neuropathy in rats. DS002 can be used in studies related to chronic pain and chemotherapy-induced peripheral neuropathy.
    DS002
  • 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-14794A
    Levomilnacipran
    		Activator
    Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
    Levomilnacipran
  • 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-181871
    DZX19
    		Inhibitor
    DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer.
    DZX19
Cat. No. Product Name / Synonyms Application Reactivity
Trk Receptor Isoform Comparison

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