2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Anaplastic lymphoma kinase (ALK)

Anaplastic lymphoma kinase (ALK)

Anaplastic lymphoma kinase; ALK tyrosine kinase receptor; CD246; Cluster of differentiation 246

Anaplastic lymphoma kinase (ALK)

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103714
    Ensartinib
    		Inhibitor 99.93%
    Ensartinib (X-396) is a BBB-permeable and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
    Ensartinib
  • HY-165422
    ALKBH5-IN-3
    		Inhibitor 99.63%
    ALKBH5-IN-3 is a selective, cell active ALKBH5 inhibitor with an IC50 of 0.021 μM. ALKBH5-IN-3 stabilizes ALKBH5 in HepG2 cells, and increases m6A level in intact cells. ALKBH5-IN-3 can be used as a versatile chemical probe to explore the biological function of ALKBH5. ALKBH5-IN-3 can be used for the research of Cancer.
    ALKBH5-IN-3
  • HY-172158
    ALKBH5-IN-5
    		Inhibitor 99.66%
    ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia.
    ALKBH5-IN-5
  • HY-13020
    GSK1838705A
    		Inhibitor 99.58%
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
    GSK1838705A
  • HY-121983
    CAY10594
    		Inhibitor 98.64%
    CAY10594 is an orally active PLD2 inhibitor with an IC50 of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.
    CAY10594
  • HY-15841
    CEP-37440
    		Inhibitor 99.91%
    CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397).
    CEP-37440
  • HY-103714A
    Ensartinib dihydrochloride
    		Inhibitor 99.73%
    Ensartinib dihydrochloride (X-396 dihydrochloride) is a BBB-permeable and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
    Ensartinib dihydrochloride
  • HY-153386
    CPD-1224
    		Inhibitor 99.83%
    CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth.
    CPD-1224
  • HY-P991504
    LAE-102
    		Antagonist 99.46%
    LAE-102 is the selective anti-ActRIIA (activin receptor type IIA or ACVR2) monoclonal antibody. LAE-102 increases muscle mass and reduces fat mass. LAE102 can increase serum activin A levels in vivo. LAE-102 is promising for research of obesity.
    LAE-102
  • HY-145574
    Iruplinalkib
    		Inhibitor 99.62%
    Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer.
    Iruplinalkib
  • HY-10432G
    A 83-01 (GMP)
    		Inhibitor
    A 83-01 (GMP) is A 83-01 (HY-10432) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. A 83-01 is a potent ALK4/5/7 inhibitor.
    A 83-01 (GMP)
  • HY-N0442
    5-O-Methylvisammioside
    		Inhibitor 99.90%
    5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.
    5-O-Methylvisammioside
  • HY-139279
    Zotizalkib
    		Inhibitor 98.02%
    Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities.
    Zotizalkib
  • HY-137506
    XST-14
    		Inhibitor 99.26%
    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
    XST-14
  • HY-P99353
    Ascrinvacumab
    		Inhibitor
    Ascrinvacumab (PF-03446962) is a human IgG2 monoclonal antibody targets ALK-1. Ascrinvacumab shows binding efficiency with human ALK1 with a Kd value of 7 nM. Ascrinvacumab can be used for the research of hepatocellular carcinoma (HCC).
    Ascrinvacumab
  • HY-123919
    TL13-112
    		Inhibitor 98.01%
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib?(HY-15656) and the Cereblon ligand of Pomalidomide (HY-10984).
    TL13-112
  • HY-148234
    M4K2234
    		Inhibitor 98.31%
    M4K2234, a chemical probe, is an orally active, highly selective inhibitor of ALK1 and ALK2 with IC50 values of 7 nM and 14 nM, respectively. M4K2234 specifically blocks BMP signaling by inhibiting the phosphorylation of SMAD1/5/8. M4K2234 inhibits BMP7-stimulated reporter gene activity (IC50 = 16 nM). M4K2234 can be used for the investigation of ALK1/2-mediated biological processes and related diseases such as diffuse midline glioma (DMG) and fibrodysplasia ossificans progressiva (FOP).
    M4K2234
  • HY-123856
    MY10
    		Activator 99.87%
    MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 reduces NF-κB p65 expression. MY10 activates tyrosine phosphorylation of c-Met. MY10 prevents the alcohol-induced downregulation of Ptprz1 and Alk expression. MY10 attenuates binge-like ethanol consumption and ethanol reward. MY10 can be used in the study of neurological and vascular diseases.
    MY10
  • HY-172240
    Tosposertib
    		Inhibitor 99.89%
    Tosposertib (TU2218 free base) is an ALK5/VEGFR2 dual inhibitor (IC50 = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer.
    Tosposertib
  • HY-17603
    Belizatinib
    		Inhibitor 99.62%
    Belizatinib (TSR-011) is an orally active, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
    Belizatinib
Cat. No. Product Name / Synonyms Application Reactivity