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DYRK

Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are conserved serine/threonine kinases. DYRKs have been implicated in cell survival, proliferation and differentiation, and in the pathology of Down Syndrome and Alzheimer's disease.

Products
Background
文献 (2)
Gene Data

DYRK Inhibitors
Cat. No. 产品名称/活性
5232 AZ 191
Potent DYRK1B inhibitor
5632 AZ Dyrk1B 33
Potent and selective Dyrk1B kinase inhibitor
7546 C28
Potent DYRK1α inhibitor; also inhibits LMTK3
6638 GSK 626616
Potent and selective DYRK inhibitor; orally bioavailable.
5075 Harmine
Potent and selective DYRK1A inhibitor
4997 INDY
DYRK1A/B inhibitor
5700 ML 315 hydrochloride
Inhibitor of Clk and DYRK kinases
7450 SGC CK2-1
Potent CK2A2 and CK2A1 inhibitor; also inhibits DYRK2
7570 T3 CLK
Potent and selective pan-CLK inhibitor; also inhibits DYRK1A/B
5088 TC-S 7004
Potent and selective DYRK1A/B inhibitor
4336 TG 003
Potent DYRK1A/B inhibitor; also inhibitor of Clk-family kinases

Related Targets

Dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are a family of serine/threonine kinases, consisting of DYRK1A, DYRK1B, DYRK2, DYRK3 and DYRK4. The DYRK family is closely related to the CMGC group of kinases (which contains CDKs, MAPKs, GSK and CLKs).

DYRKs are self-activated through auto phosphorylation of tyr-321 within the activation loop of their catalytic domain. Once activated, DYRKs phosphorylate serine and threonine residues on target proteins, which have been reported to include STAT3, Gli1, dynamin, glycogen synthase, CREB, tau and Hip-1. DYRKs can also act as priming kinases, whereby DYRK phosphorylation of a target protein enhances the efficiency of further phosphorylation by another kinase. For example DYRK1A can prime tau for further phosphorylation by GSK-1.

Physiologically DYRK1A, -1B and -3 have been implicated in cell survival, proliferation and differentiation, whereas DYRK2 is proapoptotic. The DYRK1A gene is localized to the Down Syndrome critical region of chromosome 21 and thus has been implicated in Down Syndrome pathology. Overexpression of DRYK1A in Down Syndrome neurons has been associated with the developmental defects and early onset of neurodegeneration and dementia seen in Down Syndrome. DYRK1A has also been implicated in the pathology of Alzheimer's, Parkinson's and Huntington's disease, whilst DYRK1B is over-expressed in solid tumors.

External sources of pharmacological information for DYRK :

    Literature for DYRK

    Tocris offers the following scientific literature for DYRK to showcase our products. We invite you to request* your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.

    Alzheimer's Disease Poster

    Alzheimer's Disease Poster

    Alzheimer's disease (AD) is a debilitating and progressive neurodegenerative disease and the most common cause of dementia, affecting approximately 30% of individuals aged over 85 years. This poster summarizes the cellular and molecular mechanisms of AD.

    Parkinson's Disease Poster

    Parkinson's Disease Poster

    Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.

    DYRK Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    DYRK1A Human DYRK1A NM_001396 Q13627
    Mouse Dyrk1a NM_007890 Q61214
    Rat Dyrk1a NM_012791 Q63470
    DYRK1B Human DYRK1B NM_004714 Q9Y463
    Mouse Dyrk1b NM_001037957 NP_034222
    Rat Dyrk1b NM_001107496 NP_001100966
    DYRK2 Human DYRK2 NM_003583 Q92630
    Mouse Dyrk2 NM_001014390 NP_001014412
    Rat Dyrk2 NM_001108100 NP_001101570
    DYRK3 Human DYRK3 NM_003582 O43781
    Mouse Dyrk3 NM_145508 NP_663483
    Rat Dyrk3 NM_001024767 NP_001019938
    DYRK4 Human DYRK4 NM_003845 Q9NR20
    Mouse Dyrk4 NM_207210 NP_997093.2
    Rat Dyrk4 XM_006225054 XP_006225116