DYRK

DYRK inhibitor

Dyrk1A and Dyrk1B inhibitor, selective

DYRK1B inhibitor,potent and selective

A unique regulator of PPARγ expression

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.

LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.

GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM).

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

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).

A dual inhibitor of CK2 and ERK8

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.

Potent and selective Dyrk1B kinase inhibitor

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.

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor.

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.

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.

GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 ?M for DYRK1A and GSK3β, respectively.

GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 ?M for DYRK1A and GSK3β, respectively.

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.

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.

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.