2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. DYRK

DYRK

Dual specificity tyrosine phosphorylation regulated kinase; Dual specificity tyrosine regulated kinase

DYRK

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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 Isoform Specific Products:

DYRK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    Harmine
  • HY-12277
    AZ191
    		Inhibitor 99.98%
    AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
    AZ191
  • 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.
    CLK-IN-T3
  • 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.
    GSK-626616
  • 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.
    DYRK1-IN-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.
    GSK3-IN-10
  • HY-176402
    Dyrk1A-IN-13
    		Inhibitor
    Dyrk1A-IN-13 (Compound 1) is a DYRK1A inhibitor (IC50: 41 nM). Dyrk1A-IN-13 reduces LPS-induced NO production and has antioxidant and anti-inflammatory activities. Dyrk1A-IN-13 can be used in the research of Alzheimer's disease, cancer and diabetes.
    Dyrk1A-IN-13
  • HY-173615
    KTD-092
    		Inhibitor
    KTD-092 is a hit for DYRK1A inhibition, with an IC50 of 22 nM for human DYRK1A. KTD-092 can be used in the research for Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes and other neurodegenerative diseases.
    KTD-092
  • HY-112296
    T025
    		Inhibitor 99.64%
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.
    T025
  • HY-142295
    GNF2133
    		Inhibitor 98.12%
    GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.
    GNF2133
  • HY-129492
    GNF4877
    		Inhibitor 99.78%
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
    GNF4877
  • HY-100464
    tBID
    		Inhibitor 99.03%
    tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 μM.
    tBID
  • HY-N0737
    Harmine hydrochloride
    		Inhibitor 99.98%
    Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
    Harmine hydrochloride
  • HY-108476
    INDY
    		Inhibitor 99.32%
    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.
    INDY
  • HY-U00439A
    Protein kinase inhibitor 1 hydrochloride
    		Inhibitor ≥98.0%
    Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
    Protein kinase inhibitor 1 hydrochloride
  • HY-111380
    EHT 1610
    		Inhibitor 98.16%
    EHT 1610 is a potent inhibitor of DYRK, with IC50s of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis-.
    EHT 1610
  • HY-15951
    ML167
    		Inhibitor 98.62%
    ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.
    ML167
  • 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.
    ILK-IN-3
  • HY-12838
    RO5454948
    		Inhibitor 99.53%
    RO5454948 (Compound 9) is the inhibitor for Dyrk1B and Dyrk1A with IC50 of 68 nM and 22 nM. RO5454948 exhibits cytotoxicity in cancer cell SW620 with EC50 of 1.9 μM.
    RO5454948
  • HY-146221
    Dyrk1A-IN-5
    		Inhibitor 98.56%
    Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research.
    Dyrk1A-IN-5
Cat. No. Product Name / Synonyms Application Reactivity
DYRK Isoform Comparison

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