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 small molecule inhibitor, a potent dual-specificity kinase inhibitor targeting DYRK1A (IC50=6 nM) and GSK3β (IC50=16 nM). This compound promotes β-cell proliferation by blocking NFATc nuclear export (EC50=0.66 μM for mouse R7T1 cells) and is primarily used for research on β-cell regeneration related to diabetes.

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.

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.

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

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

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.

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

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

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

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.

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

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).

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).

DYRK2-IN-1 (Compd 54) is an orally bioavailable inhibitor of DYRK2, with an IC50 of 14 nM. It can be utilized in prostate cancer research.

DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2 with an IC50 of 40.3 nM. It exhibits significantly lower inhibitory activity against DYRK1A (IC50 = 1842 nM), DYRK1B (IC50 = 1335 nM), DYRK4 (IC50 = 1931 nM), DYRK3 (IC50 = 112 nM), and CLK proteins (IC50 = 540-6496 nM). DYRK2-IN-2 hinders the phosphorylation of Tau protein at Thr212 and demonstrates moderate cytotoxicity in HT22 cells. This compound is suitable for cancer research.

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-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.