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

Trk Receptor (Trk受体)

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 相关产品 (13):

Cat. No. Product Name Effect Purity
  • HY-12497
    ANA-12 Antagonist 99.95%
    ANA-12是有效,选择性的 TrkB 拮抗剂,对高亲和力和低亲和力位点的IC50 分别为45.6 nM和41.1 μM。
  • HY-50867
    Lestaurtinib Inhibitor ≥99.0%
    Lestaurtinib (CEP-701;KT-5555) 是一种 ATP 竞争性的多激酶抑制剂,对 Trk 受体酪氨酸激酶家族具有强大的活性。 Lestaurtinib 抑制 JAK2FLT3TrkAIC50 分别为 0.9,3,小于 25 nM。
  • HY-N6732
    K-252a Inhibitor ≥99.0%
    K-252a 可从土壤真菌Nocardiopsis sp.中分离得到的一种十字孢碱的类似物,是蛋白激酶的抑制剂,对 PKC、PKA、II型钙调素依赖性激酶和磷酸化酶激酶的 IC50 值分别为470 nM、140 nM、270 nM和1.7 nM。K-252a 是一种有效抑制 NGF 受体 gp140trk 的酪氨酸蛋白激酶 (TRK) 活性,IC50 为 3 nM。
  • HY-B0527A
    Amitriptyline hydrochloride Agonist 99.56%
    Amitriptyline hydrochloride 是一种血清素再摄取转运体 (SERT) 和去甲肾上腺素再摄取转运体 (NET) 抑制剂,对人的 SERT 和 NET 作用的 Ki 值分别为 3.45 nM 和 13.3 nM。Amitriptyline hydrochloride 还与多巴胺再摄取转运体 (DAT) 结合,其 Ki 为 2.58 μM。Amitriptyline hydrochloride 也抑制肾上腺素能受体 (adrenergic receptor)、毒蕈碱受体 (muscarinic receptor )、组胺受体 (histamine receptor )、5-羟色胺受体 (5-HT receptor)。Amitriptyline hydrochloride 是一种具有强神经营养活性的 TrkATrkA 受体激动剂。Amitriptyline hydrochloride 具有抗抑郁作用。
  • HY-13491
    GNF-5837 Inhibitor ≥98.0%
    GNF-5837 是一种有效的,选择性的,口服生物利用的泛 TRK 抑制剂,在 Ba/F3 细胞中显示出抗增殖作用 (对 Tel-TrkC, Tel-TrkBTel-TrkA IC50 值分别为 7 nM,9 nM 和 11 nM)。 .
  • HY-W013372
    7,8-Dihydroxyflavone Agonist 99.90%
    7,8-Dihydroxyflavone 是有效和选择性的 TrkB 激动剂,其模拟脑源性神经营养因子 (BDNF) 的生理作用。7,8-Dihydroxyflavone 有潜力用于各种神经疾病的研究。
  • HY-17622
    Tavilermide Agonist 99.62%
    Tavilermide 是一种选择性的 TrkA 部分激动剂。
  • HY-15590
    AZ-23 Inhibitor 99.93%
    AZ-23是ATP-竞争型,有口服活性的Trk激酶 A/B/C抑制剂,IC50值分别为2 nM (TrkA),8 nM (TrkB),24 nM (FGFR1),52 nM (Flt3),55 nM (Ret),84 nM (MuSk),99 nM (Lck)。
  • HY-100673
    LM22A-4 Agonist ≥98.0%
    LM22A-4 是一种特异性的 tyrosine kinase receptor B 激动剂,常用于神经系统疾病研究。
  • HY-107854
    N-Acetyl-5-hydroxytryptamine Activator 99.86%
    N-Acetyl-5-hydroxytryptamine 是褪黑激素前体,可有效地激活 TrkB 受体。
  • HY-20878
    Tyrphostin AG 879 Inhibitor 99.54%
    Tyrphostin AG 879 (AG 879) 是一种抑制 TrKA 磷酸化 (IC50 为 10 μM) 但不抑制 TrKB 和 TrKC 的酪氨酸激酶抑制剂。Tyrphostin AG 879 还是一种选择性的 ErbB2 酪氨酸激酶抑制剂,IC50 为 1 μM,对 ErbB2 的选择性至少比 EGFR 高 500 倍。Tyrphostin AG 879 具有抗癌活性。
  • HY-129634
    TrkA-IN-1 Inhibitor
    TrkA-IN-1 是一种有效的选择性肌球蛋白相关激酶 A (TrkA) 抑制剂,在基于细胞的测定中,IC50 为 99 nM。TrkA-IN-1 具有镇痛作用。
  • HY-112436
    Trk-IN-4 Inhibitor
    Trk-IN-4 (PF-6683324 isomer) 是一种有效的 pan-Trk 抑制剂,抑制 TrkATrkBTrkC 细胞,IC50 分别为 1.9 nM,2.6 nM 和 1.1 nM。具有抗痛觉过敏作用。
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