1. Protein Tyrosine Kinase/RTK
  2. DYRK

DYRK

DYRKs (dual-specificity tyrosine-regulated kinases; dual-specificity tyrosine phosphorylation-regulated kinases) comprise a family of protein kinases within the CMGC group of the eukaryotic kinome. DYRKs contain five members in humans that are clustered into two classes based on their phylogenetic relationships: class I DYRKs, DYRK1A and DYRK1B and class II DYRKs, DYRK2, DYRK3, and DYRK4.

DYRK kinases are “dual specificity” kinases, as they can phosphorylate both tyrosine (Y) and serine/threonine (S/T) residues, although Y-phosphorylation is limited to their autophosphorylation activity. DYRK kinases phosphorylate a broad set of substrates that are involved in a wide range of cellular processes, and they are thought to fulfill essential biological functions both during development and in maintaining homeostasis during the adult life. Consequently, the aberrant regulation or expression of DYRK kinases has been associated with several human pathologies, including cancer.

DYRK Related Products (90):

Cat. No. Product Name Effect Purity
  • HY-N0737A
    Harmine Inhibitor 99.97%
    Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM[1].
  • HY-132308
    DYRK1-IN-1 Inhibitor 99.71%
    DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe[1].
  • HY-12277
    AZ191 Inhibitor 99.98%
    AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM[1].
  • HY-115470
    CLK-IN-T3 Inhibitor 98.63%
    CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity[1].
  • HY-105309
    GSK-626616 Inhibitor 99.77%
    GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia[1].
  • HY-W067583
    Norharmine Inhibitor
    Norharmine is a Harmine analogue and an alkaloid. Norharmine is the inhibitors of MAO-A and DYRK1A. Norharmine has weak inhibitory activity against MAO-A and certain inhibitory activity against DYRK1A[1].
  • HY-172198
    GSK3-IN-10 Inhibitor
    GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC50 of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress[1].
  • HY-170940
    Dyrk1A-IN-12 Inhibitor
    Dyrk1A-IN-12 (compound S43) is a Dyrk (Dual specificity tyrosine phosphorylation regulated kinase 1A inhibitor. Dyrk1A-IN-12 inhibits Dyrk1A with a IC50 of 95 nM. Dyrk1A-IN-12 shows anti-EV-A71 activity with an EC50 of 4.4 μM, CC50 of 12.8 μM and SI of 2.9. Dyrk1A-IN-12 shows potent inhibition against herpes simplex virus (HSV)[1].
  • HY-146337
    Dyrk1A/B-IN-1 Inhibitor
    Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable DYRK1A and DYRK1B inhibitor with Kis of 67.8 nM and 237.9 nM, and IC50s of 1.1 μM and 0.8 μM, respectively. Dyrk1A/B-IN-1 is not toxic to human cells. Dyrk1A/B-IN-1 can be used for researching DYRK1A and DYRK1B cellular functions and their role in pathologies[1].
  • HY-RS04101
    DYRK3 Human Pre-designed siRNA Set A Inhibitor

    DYRK3 Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

  • HY-146587
    Haspin-IN-2 Inhibitor
    Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC50 of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 445 nM and 917 nM, respectively[1].
  • HY-111379
    EHT 5372 Inhibitor
    EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively[1][2].
  • HY-168195
    DYR530
    DYR530 is a ligand for target protein (protein kinases DYRK1A) for PROTAC (HY-168194)[1].
  • HY-U00439
    Protein kinase inhibitor 1 Inhibitor
    Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-122665
    HTH-01-091 Inhibitor 98.64%
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research[1].
  • HY-115677
    ILK-IN-3 Inhibitor 99.62%
    ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model[1][2].
  • HY-108476
    INDY Inhibitor
    INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].
  • HY-101029A
    MBM-55S Inhibitor
    MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].
  • HY-34222
    7-Deazaguanine Inhibitor
    7-Deazaguanine (Compound 1) is a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor. 7-Deazaguanine is promising for research of cancers and Down’s syndrome[1].
  • HY-117049
    Leucettine L41 Inhibitor 98.70%
    Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model[2].