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

DYRK

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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0737A
    Harmine
    Inhibitor 99.88%
    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 99.68%
    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-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-117608
    ML 315
    Inhibitor
    ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.
    ML 315
  • HY-128439
    BT173
    Inhibitor
    BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway.
    BT173
  • HY-117608A
    ML 315 hydrochloride
    Inhibitor 98.75%
    ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.
    ML 315 hydrochloride
  • 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-132308
    DYRK1-IN-1
    Inhibitor 99.62%
    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-112296
    T025
    Inhibitor 98.84%
    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-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-142295
    GNF2133
    Inhibitor 98.49%
    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-12838
    Mirk-IN-1
    Inhibitor 99.53%
    Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
    Mirk-IN-1
  • HY-108476
    INDY
    Inhibitor 99.51%
    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-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-15838
    ID-8
    Inhibitor 99.16%
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
    ID-8
  • HY-111379
    EHT 5372
    Inhibitor 98.12%
    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.
    EHT 5372
  • HY-117391
    AZ-Dyrk1B-33
    Inhibitor 99.95%
    AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC50 of 7 nM.
    AZ-Dyrk1B-33
  • 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

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