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-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.
    MBM-55S
  • 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.
    Dyrk1A/B-IN-1
  • 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.
    Haspin-IN-2
  • HY-144614
    JH-XVII-10
    		Inhibitor
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.
    JH-XVII-10
  • HY-144695
    Dyrk1A/α-synuclein-IN-1
    		Inhibitor
    Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect.
    Dyrk1A/α-synuclein-IN-1
  • HY-155723
    Leucettinib-92
    		Inhibitor
    Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3).
    Leucettinib-92
  • HY-139830
    Dyrk1A-IN-1
    		Inhibitor
    Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
    Dyrk1A-IN-1
  • HY-161014
    DYRK2-IN-1
    		Inhibitor
    DYRK2-IN-1 (Compd 54) is an orally bioavailable DYRK2 inhibitor, with an IC50 of 14 nM. DYRK2-IN-1 (Compd 54) can be used in the study of prostate cancer.
    DYRK2-IN-1
  • HY-P3812
    Woodtide
    Woodtide is a substrate for the DYRK (DYRK) family of kinases whose sequence is based on that around the DYRK phosphorylation site in FKHR.
    Woodtide
  • HY-144696
    Dyrk1A/α-synuclein-IN-2
    		Inhibitor
    Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect.
    Dyrk1A/α-synuclein-IN-2
  • HY-N2892
    Aristolactam A IIIa
    		Inhibitor
    Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells.
    Aristolactam A IIIa
  • HY-144617
    JH-XIV-68-3
    		Inhibitor
    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines.
    JH-XIV-68-3
  • HY-128759
    DYRKs-IN-2
    		Inhibitor
    DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.
    DYRKs-IN-2
  • HY-129449
    AnnH31
    		Inhibitor 99.91%
    AnnH31 is a Dyrk1A inhibitor (IC50: 81 nM). AnnH31 also inhibits MAO-A with an IC50 of 3.2 μM.
    AnnH31
  • HY-77324S
    4-(Trifluoromethyl)aniline-d4
    		Inhibitor
    4-(Trifluoromethyl)aniline-d4 is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC50s of 54.84 nM and 186.40 nM, respectively[1].
    4-(Trifluoromethyl)aniline-d<sub>4</sub>
  • HY-146586
    Haspin-IN-1
    		Inhibitor
    Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC50 of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 221 nM and 916.3 nM, respectively.
    Haspin-IN-1
  • HY-142295A
    GNF2133 hydrochloride
    		Inhibitor
    GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 hydrochloride significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 hydrochloride has the potential for the research of type 1 diabetes.
    GNF2133 hydrochloride
  • HY-147760
    Dyrk1A-IN-2
    		Inhibitor
    Dyrk1A-IN-2 (Compound 63) is a DYRK1A inhibitor with an EC50 of 37 nM. Dyrk1A-IN-2 exhibits highly potent human β-cell replication-promoting activity and low cytotoxicity.
    Dyrk1A-IN-2
  • HY-152183
    FINDY
    		Inhibitor
    FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY can inhibit Ser97 autophosphorylation with an IC50 value of 35 μM. FINDY can be used for the research of neurological disorder. FINDY is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    FINDY
  • HY-122989
    Aristolactam BIII
    		Inhibitor
    Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC50= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models.
    Aristolactam BIII
DYRK Isoform Comparison

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