TrkA
TrkA (tropomyosin receptor kinase A; encoded by NTRK1) is a high-affinity receptor tyrosine kinase for nerve growth factor (NGF) that regulates neuronal survival, differentiation, and sensory neuron function through ligand-induced receptor dimerization and autophosphorylation[1][2]. Mechanistically, NGF-TrkA signaling activates major downstream pathways including RAS/MAPK, PI3K/AKT, and PLCγ, thereby controlling transcriptional programs that support neuronal growth, maintenance, and synaptic function[1][2][3]. Through these signaling cascades, TrkA plays a central role in the development and maintenance of nociceptive neurons and contributes to neurotrophin-dependent cellular responses in the peripheral and central nervous systems[1][2]. In disease contexts, dysregulation of NGF/TrkA signaling has been implicated in chronic pain disorders and neurodegenerative conditions, including experimental models of Alzheimer's disease in which impaired TrkA signaling is associated with cholinergic neuronal dysfunction and synaptic deficits[3][4][5]. Compared with related neurotrophin receptors, TrkA is distinguished by its preferential activation by NGF, whereas TrkB primarily responds to BDNF and NT-4/5 and TrkC is activated predominantly by NT-3, enabling receptor-specific biological outcomes[6]. For experimental applications, both agonists and antagonists targeting the NGF-TrkA axis have been widely utilized to investigate neurotrophic signaling, neuronal survival mechanisms, and pain-related pathways, making TrkA an important molecular target in translational neuroscience research[4][5].
References:
- [1]. Norman BH, et al. Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain. J Med Chem. 2017 Jan 12;60(1):66-88. [Content Brief]
- [2]. Indo Y. NTRK1 Congenital Insensitivity to Pain with Anhidrosis. 2008 Aug 5 [updated 2020 Apr 30]. In: Adam MP, et al. GeneReviews® [Internet]. Seattle (WA): University of Washington, Seattle; 1993–2026. PMID: 20301726. [Content Brief]
- [3]. Latina V, et al. Impaired NGF/TrkA Signaling Causes Early AD-Linked Presynaptic Dysfunction in Cholinergic Primary Neurons. Front Cell Neurosci. 2017 Mar 15;11:68. doi: 10.3389/fncel.2017.00068. PMID: 28360840; PMCID: PMC5350152. [Content Brief]
- [4]. Baño V, et al. Characterization and Structural Performance in Bending of CLT Panels Made from Small-Diameter Logs of Loblolly/Slash Pine. Materials (Basel). 2018 Nov 30;11(12):2436. [Content Brief]
- [5]. Mantyh PW, et al. Antagonism of nerve growth factor-TrkA signaling and the relief of pain. Anesthesiology. 2011 Jul;115(1):189-204. [Content Brief]
- [6]. Clinical Guidelines on the Identification, et al. National Institutes of Health. Obes Res. 1998 Sep;6 Suppl 2:51S-209S. Erratum in: Obes Res 1998 Nov;6(6):464. PMID: 9813653. [Content Brief]
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TrkA Related Products (77)
Related Products (77)
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Antibodies (4)
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Trk-IN-10
0 ImagesCat. No.: HY-144423CAS No.: 2700265-61-6Trk-IN-10 (Compound 14j) is a potent inhibitor of TRK (IC50 = 0.86, 6.92 nM, against TrkA, TrkAG595R, respectively). As a receptor tyrosine kinase (RTK), tropomyosin receptor kinase (Trk) is a key agent target in solid tumors. Trk-IN-10 (IC50 = 350 nM against ALK) has a higher selectivity of Trk inhibition, which may be of great significance for reducing toxicity.
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TRK II-IN-1
0 ImagesCat. No.: HY-151945CAS No.: 2904690-41-9
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JND4135
0 ImagesCat. No.: HY-126287CAS No.: 2366216-76-2JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model.
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Multi-kinase-IN-6
0 ImagesCat. No.: HY-156470CAS No.: 3009081-73-3Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
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Pan-Trk-IN-3
0 ImagesCat. No.: HY-144069CAS No.: 2763637-66-5Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis.
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TRK-IN-34
0 ImagesCat. No.: HY-181780CAS No.: 2489327-91-3TRK-IN-34 is an orally active TRKand TRKC mutant kinase inhibitor, with IC50 values of 0.75 nM and 0.96 nM against TRKAG595R and TRKAG667C, respectively. TRK-IN-34 inhibits the kinase activities of TRKAG595R and TRKAG667C at the functional level. TRK-IN-34 inhibits the proliferation of TRKA-transfected cells, exerts tumor growth-inhibitory effects and achieves partial tumor regression in xenograft models. TRK-IN-34 can be used to study TRK inhibitor-resistant cancers driven by the TRKAG667C mutation.
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NPA101.3
0 ImagesCat. No.: HY-183931CAS No.: 1839155-15-5NPA101.3 is an orally active RET receptor tyrosine kinase and VEGFR2 inhibitor (RET IC50 = 0.001 μM, RETV804M IC50 = 0.008 μM, VEGFR2 IC50 = 0.003 μM). NPA101.3 inhibits purified TRKA (IC50 = 32 nM) and CSF1R (IC50 = 46 nM). NPA101.3 completely suppresses tumor formation in RET/C634Y-transformed cells and also attenuates tumor formation in HRAS/G12V-transformed cells. NPA101.3 can be used in the research of RET-driven cancers.
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NTRK1-ligand-1
0 ImagesCat. No.: HY-185545CAS No.: 2922277-92-5
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Type II TRK inhibitor 1
0 ImagesCat. No.: HY-146807CAS No.: 2937543-72-9Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKAG667C and ETV6-TRKCG696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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D5261
0 ImagesCat. No.: HY-144690CAS No.: 1574574-57-4D5261 is a potent, type III allosteric tropomyosin-related kinase A (TrkA) inhibitor.
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IHMT-TRK-284
0 ImagesCat. No.: HY-146697CAS No.: 2416844-79-4
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TRK-IN-33
0 ImagesCat. No.: HY-180172TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKAG667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research.
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Anizatrectinib
0 ImagesCat. No.: HY-136535CAS No.: 1824664-89-2Synonyms: hTrkA-IN-1Anizatrectinib (hTrkA-IN-1) is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM, compound 2 extracted from patent WO2015175788. Anizatrectinib can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al.
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NMS-P626
0 ImagesCat. No.: HY-164514CAS No.: 942471-37-6NMS-P626 is an inhibitor of TRKA, TRKB, and TRKC, with IC50 values of 8 nM, 7 nM, and 3 nM, respectively. NMS-P626 inhibits the growth of KM12 cells by suppressing the phosphorylation of TPM3-TRKA and downstream signaling in KM12 cells, with an IC50 of 19 nM for KM12 cells. NMS-P626 can be used in colorectal cancer research.
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Wrightiadione
0 ImagesCat. No.: HY-N15384CAS No.: 148180-61-4Wrightiadione is a selective natural tetracyclic isoflavone kinase inhibitor with inhibitory activity against TrkA and PLK3. The IC50 values of Wrightiadione against TrkA and PLK3 are 55.8 μM and 9.0 μM, respectively. Wrightiadione is found in the dried bark of Wrightia tomentosa. Wrightiadione can be used in studies of leukemia, kinase inhibition and cancer-related signaling pathways.
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ONO-7579
0 ImagesCat. No.: HY-164517CAS No.: 1622212-25-2ONO-7579 is an orally active TRKA inhibitor that suppresses tumor growth by inhibiting the phosphorylation of TRKA. In colorectal cancer cells KM12, its EC50 is 17.6 ng/g (meaning that when each gram of tumor tissue contains 17.6 ng of ONO-7579, the activity of phosphorylated TRKA in the tumor is inhibited by 50%). ONO-7579 can be used in cancer research.
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HS-345
0 ImagesCat. No.: HY-164483CAS No.: 1462329-41-4HS-345 is a TrkA/Ak inhibitor with significant anti-pancreatic cancer effects. HS-345 inhibits the growth and proliferation of pancreatic cancer cells by targeting the TrkA/Akt signaling pathway, while also inducing apoptosis. Additionally, HS-345 suppresses blood vessel formation by decreasing the expression of HIF-1α and VEGF. HS-345 holds promise for research in pancreatic cancer.
