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Home >> Signaling Pathways >> Tyrosine Kinase >> 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.

Targets for  DYRK

Products for  DYRK

  1. Cat.No. Product Name Information
  2. GC74261 (R)-(+)-O-Demethylbuchenavianine (R)-(+)-O-Demetlbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine Chemical Structure
  3. GC74165 4-(Trifluoromethyl)aniline-d4

    4-Aminobenzotrifluoride-d4

     4-(Trifluorometl)aniline-d4 is deuterium labeled 4-(Trifluorometl)aniline. 4-(Trifluoromethyl)aniline-d4 Chemical Structure
  4. GC70625 AnnH31 AnnH31 is a Dyrk1A inhibitor (IC50: 81 nM). AnnH31 Chemical Structure
  5. GC50221 AZ Dyrk1B 33 Potent and selective Dyrk1B kinase inhibitor AZ Dyrk1B 33 Chemical Structure
  6. GC17654 AZ191 DYRK1B inhibitor,potent and selective AZ191 Chemical Structure
  7. GC72982 BT173 BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 Chemical Structure
  8. GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8 CK2/ERK8-IN-1 Chemical Structure
  9. GC73224 CLK1-IN-3 CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 Chemical Structure
  10. GC62946 DYRK1-IN-1 DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 Chemical Structure
  11. GC70985 Dyrk1A-IN-3 Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A)inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 Chemical Structure
  12. GC69031 Dyrk1A-IN-5

    Dyrk1A-IN-5 (compound 5j) is a potent and selective inhibitor of DYRK1A with an IC50 value of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits the phosphorylation of tau protein at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for research on Down syndrome.

     Dyrk1A-IN-5 Chemical Structure
  13. GC62947 DYRKs-IN-1 hydrochloride DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity. DYRKs-IN-1 hydrochloride Chemical Structure
  14. GC38330 EHT 5372 EHT 5372 Chemical Structure
  15. GC71197 FINDY FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY Chemical Structure
  16. GC64724 GNF2133 GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 ?M for DYRK1A and GSK3β, respectively. GNF2133 Chemical Structure
  17. GC64725 GNF2133 hydrochloride GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 ?M for DYRK1A and GSK3β, respectively. GNF2133 hydrochloride Chemical Structure
  18. GC38787 GNF4877 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). GNF4877 Chemical Structure
  19. GC36194 GSK-626616 GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 Chemical Structure
  20. GC30762 Harmine (Telepathine) A unique regulator of PPARγ expression Harmine (Telepathine) Chemical Structure
  21. GC38413 Harmine hydrochloride Harmine hydrochloride Chemical Structure
  22. GC72931 HTH-01-091 TFA HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA Chemical Structure
  23. GC15647 ID-8 DYRK inhibitor ID-8 Chemical Structure
  24. GC16126 INDY

    Dyrk1A and Dyrk1B inhibitor, selective

     INDY Chemical Structure
  25. GC63943 KH-CB20 KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 Chemical Structure
  26. GC33086 LDN-192960 LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively. LDN-192960 Chemical Structure
  27. GC44047 LDN-192960 (hydrochloride) LDN-192960 is an inhibitor of haspin protein kinase and dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 2 (DYRK2) with IC50 values of 10 and 48 nM, respectively. LDN-192960 (hydrochloride) Chemical Structure
  28. GC32819 Mirk-IN-1 (Dyrk1B/A-IN-1)

    Dyrk1B/A-IN-1

     Mirk-IN-1 (Dyrk1B/A-IN-1) is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively. Mirk-IN-1 (Dyrk1B/A-IN-1) Chemical Structure
  29. GC73707 ON 108600 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 Chemical Structure
  30. GC69769 Protein kinase inhibitor 1 hydrochloride

    Protein kinase inhibitor 1 hydrochloride is an effective inhibitor of HIPK2, with IC50 values of 136 and 74 nM for HIPK1 and HIPK2 respectively, and a Kd value of 9.5 nM for HIPK2.

     Protein kinase inhibitor 1 hydrochloride Chemical Structure
  31. GC34131 Protein kinase inhibitors 1 Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM. Protein kinase inhibitors 1 Chemical Structure
  32. GC61217 Protein kinase inhibitors 1 hydrochloride 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. Protein kinase inhibitors 1 hydrochloride Chemical Structure
  33. GC65395 T025

    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 Chemical Structure
  34. GC37746 tBID tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of ?0.33 ?M. tBID Chemical Structure

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