1. Protein Tyrosine Kinase/RTK
  2. DYRK

DYRK

Mammalian DYRKs are a subfamily of mitogen-activated protein kinase-related protein kinases and are originally discovered on the basis of homology to the Saccharomyces cerevisiae Yak1 and Drosophila mini-brain kinases. DYRKs possess Ser/Thr phosphorylation activity as well as autophosphorylation activity on Tyr residue(s).

Two isoforms of DYRK, DYRK1A and DYRK1B, co-immunoprecipitate with HAN11 when coexpressed in COS cells indicating that the proteins interact in mammalian cells. Co-expression of DYRK1A, DYRK1B, or DYRK2 with a series of glycogen synthase mutants with Ser/Ala substitutions at the phosphorylation sites in COS cells revealed that protein kinases cause phosphorylation of site 3a in glycogen synthase. Control of glycogen synthase by DYRK represents a novel mechanism, and a potentially novel pathway, for the regulation of glycogen synthesis.

DYRK Related Products (17):

Cat. No. Product Name Effect Purity
  • HY-N0737A
    Harmine Inhibitor 99.78%
    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[1].
  • HY-12277
    AZ191 Inhibitor 99.98%
    AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM[1].
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride Inhibitor >98.0%
    Protein kinase inhibitors 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-100464
    tBID Inhibitor >98.0%
    tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.
  • HY-15838
    ID-8 Inhibitor 99.71%
    ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.
  • HY-117391
    AZ-Dyrk1B-33 Inhibitor >99.0%
    AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC50 of 7 nM[1].
  • HY-135906
    CK2/ERK8-IN-1 Inhibitor >99.0%
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].
  • HY-105309
    GSK-626616 Inhibitor 99.83%
    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[1].
  • HY-115470
    CLK-IN-T3 Inhibitor 98.19%
    CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity[1].
  • HY-12838
    Mirk-IN-1 Inhibitor 99.53%
    Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
  • HY-129492
    GNF4877 Inhibitor 98.85%
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells)[1].
  • HY-111380
    EHT 5372 Inhibitor 98.07%
    EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.
  • HY-13455A
    LDN-192960 hydrochloride Inhibitor >98.0%
    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[1].
  • HY-U00439
    Protein kinase inhibitors 1 Inhibitor >99.0%
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-13455
    LDN-192960 Inhibitor 99.56%
    LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively[1].
  • HY-108476
    INDY Inhibitor
    INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].
  • HY-N0737
    Harmine hydrochloride Inhibitor
    Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM[1].