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Trk receptor

Trk receptors are a family of tyrosine kinases that regulates synaptic strength and plasticity in the mammalian nervous system. Trk receptors affect neuronal survival and differentiation through several signaling cascades.The common ligands of trk receptors are neurotrophins, a family of growth factors critical to the functioning of the nervous system. The binding of these molecules is highly specific. Each type of neurotrophin has different binding affinity toward its corresponding Trk receptor. The activation of Trk receptors by neurotrophin binding may lead to activation of signal cascades resulting in promoting survival and other functional regulation of cells.

Tepotinib
T61211100598-32-0
Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.
  • $35
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7,8-Dihydroxyflavone
T281638183-03-8
7,8-Dihydroxyflavone (7,8-DHF) is a naturally-occurring flavone and exist in Tridax procumbens, Godmania aesculifolia, and primula tree leaves.
  • $30
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Entrectinib
T36781108743-60-7
Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.
  • $35
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SP600125
T3109129-56-6
SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.
  • $41
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CE-245677
T14921717899-97-3
CE-245677 is a potent, reversible inhibitor of Tie2 and TrkA B kinases, with cellular IC50 values of 4.7 nM and 1 nM, respectively.
  • $56
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CG 428
T412242412055-93-5In house
CG 428 is a potent tropomyosin receptor Kinase (TRK) Degrader (uSMITETM) with a DC50 of 0.36 nM. CG 428 comprises an analog of the pan-TRK inhibitor GNF-8625 joined by a linker to the cereblon E3 ligase ligand pomalidomide. CG 428 shows selectivity for TRKA over TRKC and TRKB with Kds of 1nM, 4.2 nM, and 28 nM. CG 428 inhibits the growth of KM12 colon cancer cells with an IC50 of 2.9 nM.
  • $178
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ENT-C225
T733972919962-53-9In house
ENT-C225 is a potent TrkB neurotrophin receptor (TrkBR) activator with neuroprotective activity for the study of Alzheimer's disease and Parkinson's disease.
  • $195 TargetMol
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URMC-099
T60571229582-33-5
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
  • $52
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Larotrectinib
T59951223403-58-4
Larotrectinib (LOXO-101) is an orally administered inhibitor of the TRK kinase, demonstrating high selectivity exclusively for the TRK family of receptors (IC50s = 2-20 nM).
  • $33
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Repotrectinib
T40711802220-02-5
Repotrectinib (TPX-0005) is a potent ALK ROS1 TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.
  • $45
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Diosmetin
T1704520-34-3
Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.
  • $34
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Danusertib
T2094827318-97-8
Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.
  • $54
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ANA-12
T2359219766-25-3
ANA-12 is a potent and selective TrkB antagonist that exhibits anxiolytic and antidepressant activity in mice.
  • $34
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sitravatinib
T43491123837-84-2
Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.
  • $47
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N-Acetyl-5-hydroxytryptamine
T13541210-83-9
N-Acetyl-5-hydroxytryptamine (O-Demethylmelatonin) , also known as Normelatonin, is the immediate precursor of melatonin. It is produced from serotonin by the enzyme aralkylamine N-acetyltransferase and is converted to melatonin by acetylserotonin O-methyltransferase. It can potently activate TrkB receptor.
  • $32
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PF-06273340
T196491402438-74-7
PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflux transporters P-gp (ER = 35.7) and BCRP (ER = 4.0) and has moderate passive permeability (RRCK Papp = 5.4 × 10 6 cm s 1).
  • $77
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LM22A-4
T756837988-18-4
LM22A-4 is a brain-derived neurotrophic factor (BDNF) mimetic and agonist of the receptor tropomyosin-related kinase B (TrkB; IC50 : 47 nM in a fluorescence anisotropy assay)
  • $39
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GW 441756
T6052504433-23-2
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.
  • $51
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Lestaurtinib
T15738111358-88-4
Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.
  • $499
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Milciclib
T6081802539-81-7
Milciclib (PHA-848125) (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
  • $47
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Ensartinib hydrochloride
T223242137030-98-7
Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.
  • $60
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Belizatinib
T42571357920-84-3
Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC.
  • $36
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loxo-195
T94961350884-56-8
(6RS)-LOXO-195 (BAY 2731954) is a potent and selective Trk tyrosine kinase inhibitor.
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Taletrectinib
T223181505515-69-4
Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1 NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.
  • $68
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