dyrk1a

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.

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.

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].

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).

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 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-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].

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.

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-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-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-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-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-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.

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-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-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.

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.

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.

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.