DYRKs (dual-specificity tyrosine-regulated kinases; dual-specificity tyrosine phosphorylation-regulated kinases) comprise a family of protein kinases within the CMGC group of the eukaryotic kinome.Based on their phylogenetic relationships, DYRKs in humans have five members that are grouped into two classes: class I DYRKs, which include DYRK1A and DYRK1B, and class II DYRKs, which include DYRK2, DYRK3, and DYRK4.
Tyrosine (Y) and serine/threonine (S/T) residues can both be phosphorylated by DYRK kinases, though Y-phosphorylation is only possible through their autophosphorylation activity. DYRK kinases are believed to play crucial roles in maintaining homeostasis throughout adulthood and during development because they phosphorylate a wide variety of substrates involved in a wide range of cellular processes. As a result, several human pathologies, including cancer, have been linked to the aberrant regulation or expression of DYRK kinases.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V69711 | 4-(Trifluoromethyl)aniline-d4 (4-Aminobenzotrifluoride-d4) | 1219795-48-8 | 4-(Trifluoromethyl)aniline-d4 is the deuterated form of 4-(Trifluoromethyl)aniline. | |
V69712 | Aristolactam A IIIa (Aristolactam A IIIa; Sch 546909) | 97399-91-2 | Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid extracted from Glycosmis chlorosperma. | |
V69716 | Aristolactam BIII | 53948-10-0 | Aristolactam BIII is a potent DYRK1A inhibitor that can suppress the kinase activity of DYRK1A in vitro (IC50=9.67 nM). | |
V1954 | AZ191 | 1594092-37-1 | AZ191 is a potent and selective DYRK1B (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively. | |
V69717 | BT173 | 2232180-74-2 | BT173 is a potent homeodomain-interacting protein kinase 2 (HIPK2) inhibitor. | |
V69705 | DYRK1-IN-1 | 2814486-79-6 | DYRK1-IN-1 is a selective and ligand-efficient DYRK1A inhibitor. | |
V69715 | Dyrk1A-IN-1 | 2858696-72-5 | Dyrk1A-IN-1 is a tripartite inhibitor of Dyrk1Kinase activity (IC50 = 119 nM), aggregation of tau and α-syn oligomers. | |
V84259 | Dyrk1A-IN-6 | |||
V88015 | Dyrk1A-IN-7 | Dyrk1A-IN-7 (Compound 29) is a selective DYRK1A kinase inhibitor with good kinase selectivity over CLK1 kinase, with an IC50 of 28 nM for DYRK1A and a Kd of 17.5 nM for CLK2. | ||
V88016 | Dyrk1A-IN-8 | 101578-13-6 | Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A with IC50 of 209 nM. | |
V88018 | Dyrk1A-IN-9 | Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC50: 1.67 μM). | ||
V69719 | Dyrk1A/α-synuclein-IN-1 | 2789711-47-1 | Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual (bifunctional) inhibitor of Dyrk1A and α-synuclein aggregation with IC50s of 177 nM and 10.5 µM, respectively. | |
V69707 | Dyrk1A/α-synuclein-IN-2 | 2789711-66-4 | Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual (bifunctional) inhibitor of Dyrk1A and α-synuclein aggregation with IC50 of 7.8 µM for α-synuclein. | |
V85608 | DYRK2-IN-1 | |||
V69710 | DYRKs-IN-1 hydrochloride | 1386980-55-7 | DYRKs-IN-1 HCl is a potent inhibitor of DYRKs (dual-specificity tyrosine phosphorylation-regulated kinases) with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. | |
V20428 | EHT-1610 | 1425945-60-3 | EHT-1610 is a novel, potent and selective DYRK kinase inhibitor with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively. | |
V69713 | FINDY | 1507367-37-4 | FINDY is an intermediate-fold selective inhibitor of DYRK1A. | |
V69703 | GNF2133 | 2561414-56-8 | GNF2133 is a specific, orally bioactive DYRK1A inhibitor (antagonist) with IC50 of 0.0062 and >50 µM for DYRK1A and GSK3β, respectively. | |
V21894 | GSK-626616 | 1025821-33-3 | GSK 626616 is a novel, potent, and orally bioavailable YAK3/DYRK3 kinase inhibitor with IC50of 0.7 nM for DYRK3. | |
V1953 | ID-8 | 147591-46-6 | ID-8 is a novel and potent small molecule DYRK (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor that sustains embryonic stem cell self-renewal in long-term culture. |