2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. DYRK
  5. DYRK4 Isoform

DYRK4

Dual specificity tyrosine-phosphorylation-regulated kinase 4 (DYRK4) is a serine/threonine kinase with limited tissue expression, predominantly in stage VIII postmeiotic spermatids[1]. Mechanistically, DYRK4 participates in phosphorylation-mediated regulation of transcription factors, contributing to the fine-tuning of spermiogenesis, although knockout models indicate functional redundancy among DYRK isoforms[1]. Multiple splice variants of DYRK4 exhibit distinct subcellular localizations and enzymatic activities, including a nuclear-localized variant that interacts with importin α3/α5, and a cytoplasmic variant with reduced catalytic activity due to a three-amino-acid deletion in subdomain XI[2]. DYRK4 differs from other DYRK family members in substrate specificity, as it lacks the arginine P-3 preference characteristic of DYRK1A, highlighting isoform-specific functional divergence[2]. Experimental modulation of DYRK4 activity has been explored using selective DYRK inhibitors developed for related isoforms, with potential utility in dissecting isoform-specific roles in cell differentiation and metabolic regulation[3][4][5]. Although no disease phenotype is directly associated with DYRK4 deficiency, its restricted expression and splice-dependent activity suggest applications as a model for investigating testis-specific kinase regulation and isoform-selective therapeutic targeting[1][2].

DYRK4 Related Products (6):

Cat. No. Product Name Effect Purity
  • 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-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.
  • HY-122665
    HTH-01-091
    		Inhibitor 99.81%
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.
  • 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.