dyrk1a

Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable inhibitor of DYRK1A and DYRK1B. Dyrk1A/B-IN-1 inhibits 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-IN-1 is a triple inhibitor of Dyrk1A kinase activity, aggregation of tau and α-syn oligomers, with an IC50 value of 119 nM for Dyrk1A kinase.

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

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

Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual inhibitor of Dyrk1A and α-synuclein aggregation that acts on α-synuclein (IC50: 7.8 μM). Dyrk1A/α-synuclein-IN-2 has a high predictive CNS permeability and neuroprotective effect.

Dyrk1A-IN-3 (Compound 8b) is a highly selective inhibitor of dual-specificity tyrosine-regulated kinase 1A (DYRK1A). Dyrk1A-IN-3 has high binding affinity of DYRK1A with an IC 50 of 76 nM. Dyrk1A-IN-3 can be used in neurodegenerative disorders research, for example, Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease [1].

Dyrk1A-IN-5 (compound 5j) is a highly potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 6 nM. It dose-dependently diminishes the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Moreover, Dyrk1A-IN-5 effectively inhibits the phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Given these properties, Dyrk1A-IN-5 is a valuable tool 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.

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).

TBCA (Casein Kinase II Inhibitor III, TBCA) is a highly selective CK2 (casein kinase II) inhibitor, IC50 = 110 nM, Ki = 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

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].

NU6102 is a selective and potent ATP-competitive CDK2 inhibitor with antitumor activity against CDK1 cyclinB, CDK2 cyclinA3, CDK1 CDK2, CDK4, DYRK1A , PDK1, and ROCKII, and it can be used to study rectal cancer.

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.

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).

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.

Palbociclib D8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active inhibitor of CDK4 and CDK6 (IC50s of 11 and 16 nM, respectively).

ZDWX-25 is a highly potent dual inhibitor of GSK-3β and DYRK1A that possesses significant cytotoxic activities towards SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for Alzheimer's disease research with an IC 50 value of 71 nM for GSK-3β [1].

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.

Paprotrain ((alphaZ)-alpha-(3-Pyridinylmethylene)-1H-indole-3-acetonitrile) inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM.

JH-XVII-10 is a selective, orally active and potent inhibitor of DYRK1A (IC50: 3 nM) and DYRK1B (IC50: 5 nM).JH-XVII-10 exhibits antitumor effects in squamous cell carcinoma of the neck (HNSCC) cell lines.

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.

GNF7156 is a potent and selective DYRK1A inhibitor.

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

Mirk-IN-1 is an effective inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A (IC50: 68±48 nM and 22±8 nM respectively).

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.

GNF4877 is a potent DYRK1A and GSK3β inhibitor (IC50s: 6 nM and 16 nM). It leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation cells.

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability that can be used for the research of central nervous system penetrant DYRK1A chemical probe [1].

Haspin-IN-1 (compound 2a) is an inhibitor of haspin (haploid germ cell-specific nuclear protein kinase) with an IC50 of 119 nM. Haspin-IN-1 also inhibits CLK1, DYRK1A, and CDK9 with IC50 of 221 nM, 916.3 nM, and 406.8 nM, respectively. Haspin-IN-1 has the potential for the development of new anticancer drugs [1].

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.

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.

FINDY, an inhibitor selective for the folding intermediate of DYRK1A, effectively blocks Ser97 autophosphorylation, exhibiting an IC50 of 35 μM. This compound is utilized in neurological disorder research.

KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and CLK4 , with an IC 50 of 16.5 nM for CLK1 . KH-CB20 also can inhibits DYRK1A ( IC 50 =57.8 nM) and CLK3 ( IC 50 =488 nM).

Haspin-IN-2 (compound 4) is a potent, selective inhibitor of haspin, exhibiting an IC50 of 50 nM. Additionally, it inhibits CLK1 and DYRK1A, with IC50 values of 445 nM and 917 nM, respectively [1].

ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.028 μM for DYRK2, 0.05 μM and 0.005 μM for CK2α1 and CK2α2, and 0.005 μM for TNIK, respectively. This compound exhibits antitumor activity [1].

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

Palbociclib (PD 0332991) orotate, an orally active selective inhibitor of CDK4 and CDK6, exhibits IC50 values of 11 and 16 nM, respectively. This compound demonstrates potent anti-proliferative effects and induces cell cycle arrest in cancer cells, applicable in research concerning HR-positive, HER2-negative breast cancer, and hepatocellular carcinoma [1] [3] [4].

JH-XIV-68-3 is a selective inhibitor of the DYRK1A/B macrocycle.JH-XIV-68-3 selectively acts on DYRK1A and its close relative DYRK1B in biochemical and cellular assays.JH-XIV-68-3 has antitumor effects in head and neck squamous cell carcinoma (HNSCC) cell lines.

AChE/GSK-3β-IN-1 is a potent dual AChE/GSK-3β inhibitor that crosses the blood-brain barrier and acts on hAChE (IC50: 1.2 nM), hBChE (IC50: 149.8 nM) and hGSK-3β (IC50: 22.4 nM). AChE/GSK-3β-IN-1 is able to occupy the ATP binding site of DYRK1A. aChE/GSK-3β-IN-1 exhibits high kinase selectivity for the CMGC kinase family. aChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. aChE/GSK-3β-IN-1 can be used to study Alzheimer's disease.

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.

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

Harmalol hydrochloride (Harmidol hydrochloride) is a β-carboline alkaloid that can be extracted from the seeds of Peganum harmala L. Harmalol hydrochloride is the major metabolite of Harmaline and significantly inhibits dioxin-mediated induction of CYP1A1 at both transcriptional and post-translational levels. Harmalol hydrochloride showed vasorelaxant activity in isolated rat thoracic aortic preparations preconstricted with phenylephrine or KCl. Harmalol hydrochloride has antioxidant activity.

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

KH-CB19 is an effective and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).

EHT 5372 is a potent and selective inhibitor of DYRK’s family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2， DYRK3， CLK1, CLK2, CLK4, GSK-3α, GSK-3β.

GNF2133 hydrochloride is a selective, effective, and orally active DYRK1A inhibitor, able to act on DYRK1A (IC50: 0.0062 μM) and GSK3β (IC50> 50 μM); GNF2133 hydrochloride showed good proliferative ability and efficacy in rat and human primary β cells. GNF2133 hydrochloride significantly improved glucose processing ability and increased insulin secretion. GNF2133 hydrochloride has the potential to study type 1 diabetes.

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.

Palbociclib (PD 0332991) dihydrochloride is an orally active, selective inhibitor of CDK4 (IC50: 11 nM) and CDK6 (IC50: 16 nM). Palbociclib dihydrochloride has anti-proliferative activity and cell cycle arrest in HR-positive and HER2-negative breast cancers, as well as in hepatocellular carcinoma studies.

Palbociclib (PD 0332991) hydrochloride is a selective and potent inhibitor of CDK4 (IC50: 11 nM) and CDK6 (IC50: 16 nM). Palbociclib hydrochloride has anti-proliferative effects on cancer cells and induces cell cycle arrest, and can be used in research on HR-positive and HER2-negative breast cancer, as well as hepatocellular carcinoma.

Palbociclib monohydrochloride (PD 0332991 hydrochloride) is a selective inhibitor of CDK4/6 (IC50s: 11/16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Palbociclib Isethionate (PD 0332991 isethionate) is a selective inhibitor of CDK4 6 (IC50s: 11 16 nM). It exhibits no inhibition against a panel of 36 additional protein kinases.