2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. DYRK
  5. DYRK3 Isoform

DYRK3

DYRK3 (dual-specificity tyrosine phosphorylation-regulated kinase 3) functions as a serine/threonine and tyrosine kinase involved in cellular stress responses and proteostasis[1]. Mechanistically, DYRK3 phosphorylates components of stress granules and liquid-liquid phase separation structures, thereby regulating protein solubility and phase transition during nutrient deprivation or hypoxic stress[1]. In disease models, DYRK3 activity influences tumor cell survival by controlling proteasome function and modulating key transcription factors, including heat-shock factor 1 and c-Myc[1]. Compared with related isoforms such as DYRK1A and DYRK2, DYRK3 exhibits a distinct cytoplasmic localization and preferential engagement with stress granule substrates rather than nuclear transcriptional regulators[1][2]. Small-molecule inhibitors of DYRK3, characterized by high selectivity within the CMGC kinase family, have demonstrated the ability to disrupt stress-mediated proteostasis and reduce tumor cell proliferation in preclinical studies[3][4]. These inhibitors, often based on pyrimidine or imidazopyridazine scaffolds, facilitate mechanistic studies and provide a foundation for experimental applications targeting DYRK3-dependent pathways[3][4]. Overall, DYRK3 serves as a regulatory kinase coordinating cellular adaptation to environmental stress, distinguishing itself from other DYRK isoforms through substrate specificity and cytoplasmic function, with emerging potential for therapeutic intervention[2][1].

DYRK3 Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-105309
    GSK-626616
    		Inhibitor 99.88%
    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.
  • HY-117049
    Leucettine L41
    		Inhibitor 98.98%
    Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). Leucettine L41 can also inhibit GSK-3 singnaling. Leucettine L41 can inhibit cell apoptosis and ROS production. Leucettine L41 can promote β-cell cell cycle progression, cell proliferation and increase insulin secretion. Leucettine L41 can be used for the researches of neurological disease and metabolic disease, such as Alzheimer’s disease (AD) and diabetes.
  • HY-162750
    ZJCK-6-46
    		Inhibitor 99.06%
    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.
  • HY-402805
    DYRK2-IN-2
    		Inhibitor
    DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC50 value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLKs (IC50 = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research.
  • HY-402805A
    DYRK2-IN-2 hydrochloride
    		Inhibitor
    DYRK2-IN-2 hydrochloride is a selective DYRK2 inhibitor with an IC50 of 40.3 nM. DYRK2-IN-2 hydrochloride shows weaker inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM) and CLK (IC50 = 540-6496 nM). DYRK2-IN-2 hydrochloride inhibits the phosphorylation of Thr212 in Tau protein. DYRK2-IN-2 hydrochloride is applicable for neuronal research.