1. Signaling Pathways
  2. Protein Tyrosine Kinase/RTK
  3. ALK

ALK (间变性淋巴瘤激酶)

Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase in the insulin receptor superfamily, is predominantly expressed in the brain and implicated in neuronal development and cognition. ALK catalyzes the transference of a gamma-phosphate group from adenosine triphosphate (ATP) to a tyrosine residue on a substrate protein. Therefore, it catalyzes a tyrosine residue phosphorylation reaction on its substrate proteins. The phosphorylation and dephosphorylation of proteins are critical reactions catalyzed by different enzymes (kinases and phosphatases), which play critical roles in various cellular functions.

ALK gene activation is involved in the carcinogenesis process of several human cancers such as anaplastic large cell lymphoma, lung cancer, inflammatory myofibroblastic tumors and neuroblastoma, as a consequence of fusion with other oncogenes (NPM, EML4, TIM, etc) or gene amplification, mutation or protein overexpression. ALK is a transmembrane tyrosine kinase receptor that, upon ligand binding to its extracellular domain, undergoes dimerization and subsequent autophosphorylation of the intracellular kinase domain. When activated in cancer it represents a target for specific inhibitors, such as Crizotinib, Ceritinib, Alectinib etc. which use has demonstrated significant effectiveness in ALK-positive non-small cell lung cancer particularly.

ALK 相关产品 (16):

目录号 产品名 作用方式 纯度
  • HY-10432
    A 83-01 Inhibitor ≥98.0%
    A 83-01 是一种有效的 TGF-β I 型受体 ALK5ALK4ALK7 的抑制剂,能够抑制 ALK5ALK4ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。
  • HY-10432A
    A 83-01 sodium salt Inhibitor
    A 83-01 sodium salt 是一种有效的 TGF-β I 型受体 ALK5ALK4ALK7 的抑制剂,能够抑制 ALK5ALK4ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。
  • HY-15609
    AZD-3463 Inhibitor 99.96%
    AZD-3463 (ALK/IGF1R inhibitor) 是一种具有口服活性的 ALK/IGF1R 抑制剂,对 ALK 作用的 Ki 值为 0.75 nM。AZD-3463 可诱导神经母细胞瘤细胞凋亡 (apoptosis) 和自噬 (autophagy)。
  • HY-15357
    ALK inhibitor 1 Inhibitor 99.71%
    ALK inhibitor 1 (compound 17) 是一种有效的,嘧啶类 ALK 抑制剂。ALK inhibitor 1 是有效的睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2; IC50=31 nM) 和粘着斑激酶 (FAK; IC50=2 nM) 抑制剂。
  • HY-16590
    X-376 Inhibitor 98.36%
    X-376 是一种有效的高特异性 ALK 酪氨酸激酶抑制剂 (TKI) (IC50=0.61 nM)。X-376 是 MET 的较低效抑制剂 (IC50=0.69 nM)。X-376 具有有效的抗肿瘤活性。
  • HY-130794
    ALK/ROS1-IN-1 Inhibitor
    ALK/ROS1-IN-1 (compound 2e) 是一种高效、选择性的抗 crizotinib 耐受 ALK/ROS1 双重抑制剂,对 ALK 和 ROS1 酶作用的 IC50 值分别为 0.174 μM 和 0.530 μM。
  • HY-15358
    ALK inhibitor 2 Inhibitor 99.77%
    ALK inhibitor 2 (compound 18) 是一种有效的,嘧啶类 ALK 抑制剂。ALK inhibitor 2 是有效的睾丸特异性丝氨酸/苏氨酸激酶 2 (TSSK2; IC50=37 nM) 和粘着斑激酶 (FAK; IC50=5 nM) 抑制剂。
  • HY-15801
    HG-14-10-04 Inhibitor 98.83%
    HG-14-10-04 (example 10) 是特异的 ALK 抑制剂,IC50 为 20 nM。
  • HY-N4126
    6-Demethoxytangeretin Inhibitor 99.28%
    6-​Demethoxytangeretin 6-去甲氧基三苯甲基黄嘌呤是从柑橘 (Citrus depressa) 分离的黄酮。 6-Demethoxytangeretin 具有抗炎和抗过敏活性,通过间变性淋巴瘤激酶 (ALK) 和丝裂原活化蛋白激酶 (MAPK) 途径抑制人肥大细胞中 IL-6 的产生和基因表达。6-​Demethoxytangeretin 促进 CRE 介导的转录 (与海马神经元的学习和记忆相关)。
  • HY-112140
    JH-VIII-157-02 Inhibitor 98.86%
    JH-VIII-157-02 是 alectinib 的结构类似物,为 ALK 抑制剂,对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。
  • HY-112801
    F-1 Inhibitor
    F-1 是一种有效的 ALKROS1 的双重抑制剂,抑制 ALK 的磷酸化及下游通路,对 ALKWT,ROS1WT,ALKL1196M 和 ALKG1202RIC50 值分别为 2.1 nM,2.3 nM,1.3 nM 和 3.9 nM。
  • HY-125851
    TP-008 Inhibitor
    TP-008 是一种有效的,选择性的和口服活性的激活素样激酶 5 (ALK 5) 抑制剂,pIC50pEC50 值分别为 7.6 和 6.63。TGFβRI-IN-2 在高剂量时会在体内产生心脏毒性。
  • HY-136194
    TL13-22 Inhibitor
    TL13-22 是 一种 TL13-12 (HY-122582) 的阴性对照,是一种有效的 ALK 抑制剂,IC50 为 0.54 nM。TL13-22 不会降解细胞中的 ALK
  • HY-136195
    TL13-110 Inhibitor
    TL13-110 是 一种 TL13-112 (HY-123919) 的阴性对照,是一种有效的 ALK 抑制剂,IC50 为 0.34 nM。TL13-110 不会降解细胞中的 ALK
  • HY-103714
    Ensartinib Inhibitor
    Ensartinib (X-396) 是一种有效的双重的 ALK/MET 抑制剂,IC50 分别 <0.4 nM 和 0.74 nM。
  • HY-111416
    WY-135 Inhibitor
    WY-135是ALK (IC50=1.4 nM) 和 ROS1 (IC50=1.1 nM) 的双抑制剂。
Isoform Specific Products

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