dual specificity tyrosine regulated kinase

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.

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.

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.

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.

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

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).

LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin, with IC50 values of 48 nM and 10 nM, respectively.

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].

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].