dyrk1a

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).

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.

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.

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).

Palbociclib-d8 (PD 0332991 D8) is the 2H-labeled form of Palbociclib. Palbociclib is an orally active CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM). Palbociclib has anti-tumor activity and is used in research for estrogen receptor-positive and HER2-negative breast cancer.

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.

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.

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.

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.

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

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.

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].

Dyrk1A-IN-11 (compound 166) is an effective inhibitor targeting dual-specificity tyrosine phosphorylation-regulated 1A (DYRK1A) with an EC50 of 0.0021 µM. Additionally, this compound inhibits the phosphorylation of Tau (Thr212) with an EC50 of 0.0361 µM.

Dyrk1A-IN-12 (compound S43) is an inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1A). It has an IC50 of 95 nM for inhibiting Dyrk1A. The compound demonstrates antiviral activity against EV-A71 (Enterovirus A71) with an EC50 of 4.4 μM, a CC50 of 12.8 μM, and a selectivity index (SI) of 2.9. Additionally, Dyrk1A-IN-12 exhibits potent inhibitory effects on the herpes simplex virus (HSV).

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].

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-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 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-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.

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-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-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-IN-8 is an active molecule that can be used in life science related research. The CAS number of Dyrk1A-IN-8 is 101578-13-6.

Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor noted for its anti-diabetic activity. It enhances pancreatic beta-cell proliferation, boosts insulin secretion, and lowers blood glucose levels.