DYRK

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

YK-2-69 is a highly selective DYRK2 inhibitor with anti-prostate cancer effects.

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

ProINDY (Pro-indy) is a potent DYRK inhibitor that activates NFAT for the study of Down syndrome.

ML 315 is a selective Clk and DYRK inhibitor with potential anticancer activity for the study of neurological disorders.

AnnH31 is a potent Dyrk1A inhibitor with an IC50 value of 81 nM.AnnH31 inhibits MAO-A with an IC50 of 3.2 μM.AnnH31 can be used as a probe to confirm the involvement of DYRK1A in cellular phosphorylation.

ARN25068 is a potent inhibitor of GSK-3β, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.

AZ191（IC50 of 17 nM） is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

ID-8, a DYRK inhibitor, sustains embryonic stem cell self-renewal in long-term culture.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.

INDY is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50s of 0.24 μM and 0.23 μM and a Ki of 0.18 μM for Dyrk1A ATP pocket, respectively.

ML167 (CID44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

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

Harmine hydrochloride (telepathine hydrochloride) is extracted from Peganum Harmala Genus.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

Dyrk1A-IN-4 (compound 48) is a potent and orally active dual inhibitor of DYRK1A (IC50 = 2 nM) and DYRK2 (IC50 = 6 nM) with anticancer effects [1].

Dyrk1A B-IN-1 (compound 3n) is a potent, selective, and cell-permeable inhibitor of DYRK1A and DYRK1B, with Kis of 67.8 nM and 237.9 nM, and IC 50 s of 1.1 μM and 0.8 μM, respectively.

Dyrk1A α-synuclein-IN-2 (Compound b20) is a dual inhibitor of Dyrk1A and α-synuclein aggregation with an IC50 of 7.8 μM for α-synuclein. It exhibits high predictive CNS permeability and has a neuroprotective effect.

Dyrk1A-IN-3 (Compound 8b) is a highly selective inhibitor of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) with a high binding affinity (IC50 of 76 nM). Dyrk1A-IN-3 can be used in neurodegenerative disorders research, such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease [1].

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor that inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. It exhibits good permeability and cellular activity without P-glycoprotein liability, making it suitable for research on central nervous system penetrant DYRK1A chemical probes [1].

Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity, tau aggregation, and α-syn oligomers, with an IC50 value of 119 nM for Dyrk1A kinase.

Dyrk1A-IN-5 (compound 5j) is a highly potent and selective DYRK1A inhibitor with an IC50 of 6 nM, reducing the phosphorylation of Thr434 in SF3B1 dose-dependently (IC50 = 0.5 μM) and inhibiting tau phosphorylation at Thr212 (IC50 = 2.1 μM), making it valuable for Down syndrome research [1].

Dyrk1A-IN-2 is a DYRK1A inhibitor (EC50: 37 nM). dyrk1A-IN-2 exhibits efficient promotion of human β-cell replication, as well as low cytotoxicity.

Dyrk1A α-synuclein-IN-1 (Compound b1) is a dual inhibitor of Dyrk1A (IC50: 177 nM) and α-synuclein aggregation (IC50: 10.5 μM), characterized by CNS permeability and neuroprotective activity.

DYRKs-IN-1 hydrochloride is a potent inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), with IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B, and exhibits antitumor activity.

DYRKi is a nontoxic, DYRK1-selective inhibitor.

Potent and selective CLK inhibitor (IC50 values are 28, 88 and 510 nM for CLK4, 1 and 2, respectively). Exhibits no significant activity at CLK3, DYRK, CDK or GSK3 at a concentration of 10 μM. Inhibits growth of a range of cancer cell lines in vitro at subnanomolar concentrations. Walter et al (2018) Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. PLoS One 13 e0196761 PMID:29723265

Woodtide, a substrate for the DYRK (DYRK) family of kinases, is designed based on the sequence surrounding the DYRK phosphorylation site in FKHR [1] [2].

Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK CLK families, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3 [1].

ML 315, a selective dual inhibitor targeting CDK (Cyclin-Dependent Kinase) and DYRK (Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase) with IC50 values of 68 nM and 282 nM, respectively, is utilized in research pertaining to cancer and neurological diseases [1].