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
- Cat.No. Product Name Information
- GC50221 AZ Dyrk1B 33 Potent and selective Dyrk1B kinase inhibitor
- GC17654 AZ191 DYRK1B inhibitor,potent and selective
- GC39485 CK2/ERK8-IN-1 A dual inhibitor of CK2 and ERK8
- GC62946 DYRK1-IN-1 DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor.
- 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.
- GC38330 EHT 5372
- GC64724 GNF2133 GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 ?M for DYRK1A and GSK3β, respectively.
- 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.
- 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).
- GC36194 GSK-626616 GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM).
- GC30762 Harmine (Telepathine) A unique regulator of PPARγ expression
- GC38413 Harmine hydrochloride
- GC15647 ID-8 DYRK inhibitor
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GC16126
INDY
Dyrk1A and Dyrk1B inhibitor, selective
- 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.
- 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.
- 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.
- GC38403 LDN-192960 hydrochloride 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.
- GC32819 Mirk-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.
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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.
- 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.
- 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.
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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.
- GC37746 tBID tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of ?0.33 ?M.