2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. DYRK
  5. DYRK2 Isoform

DYRK2

DYRK2 (dual-specificity tyrosine-phosphorylation-regulated kinase 2) is a member of the DYRK kinase family that integrates cell-cycle control, DNA-damage signaling, proteostasis, and apoptosis through substrate-specific phosphorylation events[1][2]. Upon genotoxic stress, DYRK2 undergoes nuclear translocation and directly phosphorylates p53 at Ser46, promoting p53-dependent apoptotic transcriptional programs and irreversible cell-fate commitment after severe DNA damage[1]. Mechanistically, ATM-dependent phosphorylation stabilizes DYRK2 and supports its accumulation in the nucleus, linking DNA-damage sensing to apoptotic execution pathways[3]. Beyond p53 regulation, DYRK2 functions as a priming kinase for c-Jun and c-Myc, facilitating their ubiquitination and degradation, thereby influencing G1/S cell-cycle progression and oncogenic signaling networks[4]. DYRK2 also regulates proteostasis by phosphorylating the 26S proteasome and enhancing proteasome activity, a process associated with survival of proteasome-dependent tumor cells including multiple myeloma and triple-negative breast cancer models[5][6]. In disease settings, altered DYRK2 expression has been associated with tumor progression, chemosensitivity, and metastatic behavior, although its biological role remains context dependent across cancer types[2][7]. Compared with related DYRK isoforms, DYRK2 is distinguished by its prominent regulation of p53-dependent apoptosis, proteasome activation, and ubiquitin-mediated turnover of oncogenic substrates[1][4][5]. For experimental applications, pharmacological inhibition of DYRK2 suppresses proteasome activity and impairs growth of proteasome-addicted cancers, supporting its value as a mechanistic target in translational oncology research[6][8].

DYRK2 Related Products (21):

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-112296
    T025
    		Inhibitor 99.64%
    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.
  • 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.
  • 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-146221
    Dyrk1A-IN-5
    		Inhibitor 98.06%
    Dyrk1A-IN-5 (Compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC50 = 600 nM) and CLK1 (IC50 = 500 nM), but shows almost no inhibition of DYRK2 (IC50 > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research.
  • 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.
  • HY-153949
    YK-2-69
    		Inhibitor 99.57%
    YK-2-69 is a highly selective DYRK2 inhibitor with an IC50 value of 9 nM. YK-2-69 specifically interacts with Lys-231 and Lys-234 of DYRK2 and can be utilized in researches related to prostate cancer.
  • HY-147066
    Dyrk1A-IN-4
    		Inhibitor 99.30%
    Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC50s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC50 of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma.
  • HY-125290
    MU1210
    		Inhibitor 99.50%
    MU1210 (compound 12f), a chemical probe, is an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 (with IC50 values of 8, 20, and 12 nM respectively), with IC50 for HIPK1 and DYRK2 are 187 and 1309 nM. MU1210 also has favorable pharmacokinetic characteristics (in mice, 10 mg/kg, intraperitoneal injection: Cmax=1.24 μM, T1/2=58 minutes; no acute toxicity observed).
  • 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-156816
    ON 108600
    		Inhibitor 98.65%
    ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity.
  • HY-13455
    LDN-192960
    		Inhibitor 99.58%
    LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-110320
    LDN-209929 dihydrochloride
    		Inhibitor 98.33%
    LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).
  • 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-13455A
    LDN-192960 hydrochloride
    		Inhibitor 99.76%
    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.
  • HY-161597
    PROTAC DYRK2 degrader 1
    		Degrader
    PROTAC DYRK2 degrader 1 is a DYRK2 PROTAC degrader with DC50 values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer.
  • 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.
  • HY-161598
    DYRK2 ligand 1
    		Degrader
    DYRK2 ligand 1 is a target protein ligand of PROTAC DYRK2 degrader 1 (HY-161597). DYRK2 ligand 1 can be used to study cancer.
  • HY-177416
    MU1787
    		Inhibitor
    MU1787 is a highly selective homeodomain-interacting protein kinase (HIPK) inhibitor with a furopyridine core, and shows improved selectivity against CLKs, with inactivity against DYRK1B, DYRK2, and MLK2/3 in in vitro cellular assays. MU1787 can be used for the research of malignancies.