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-N12625
    (R)-(+)-O-Demethylbuchenavianine
    		Inhibitor 98.67%
    (R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC50s of 1.1, 0.95, >10, >10 and >10 μM, respectively.
    (R)-(+)-O-Demethylbuchenavianine
  • HY-RS04095
    Dyrk1a Mouse Pre-designed siRNA Set A
    		Inhibitor

    Dyrk1a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Dyrk1a Mouse Pre-designed siRNA Set A
  • HY-13455A
    LDN-192960 hydrochloride
    		Inhibitor 99.78%
    LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
    LDN-192960 hydrochloride
  • 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-U00439
    Protein kinase inhibitor 1
    		Inhibitor ≥99.0%
    Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
    Protein kinase inhibitor 1
  • 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-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-X0009A
    Tambiciclib dimaleate
    		Inhibitor
    Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research.
    Tambiciclib dimaleate
  • HY-162750
    ZJCK-6-46
    		Inhibitor
    ZJCK-6-46 (32) is a potential and orally activeDYRK1A inhibitor (IC50 = 0.68 nM) with high BBB permeability (CNS+). ZJCK-6-46 (32) reduces tau phosphorylation. ZJCK-6-46 (32) ameliorates cognitive dysfunction by obviously reducing the expression of phosphorylated tau and neuronal loss in vivo.
    ZJCK-6-46
  • HY-128758
    DYRKs-IN-1
    		Inhibitor
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.
    DYRKs-IN-1
  • HY-122665A
    HTH-01-091 TFA
    		Inhibitor 99.48%
    HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.
    HTH-01-091 TFA
  • HY-N0737AR
    Harmine (Standard)
    		Inhibitor
    Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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.
    DYRK3 Human Pre-designed siRNA Set A
  • 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-168195
    DYR530
    DYR530 is a ligand for target protein (protein kinases DYRK1A) for PROTAC (HY-168194).
    DYR530
  • HY-RS04096
    Dyrk1a Rat Pre-designed siRNA Set A
    		Inhibitor

    Dyrk1a Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Dyrk1a Rat Pre-designed siRNA Set A
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
DYRK Isoform Comparison

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