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 |
|---|---|---|---|---|
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V69711 | 4-(Trifluoromethyl)aniline-d4 (4-Aminobenzotrifluoride-d4) | 1219795-48-8 | 4-(Trifluoromethyl)aniline-d4 is the deuterated form of 4-(Trifluoromethyl)aniline. |
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V105504 | 7-Deazaguanine | 7355-55-7 | 7-Deazaguanine (compound 1) is a highly selective, well-tolerated, and brain-penetrating DYRK1A inhibitor. |
|
V114763 | AO-365/43472821 | 1081122-55-5 | AO-365/43472821 is a highly selective, blood-brain barrier-crossing, bispecific tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM), which also exhibits significant inhibitory activity against CLK1 (IC50 = 0.08 μM). |
|
V69712 | 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. |
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V69705 | DYRK1-IN-1 | 2814486-79-6 | DYRK1-IN-1 is a selective and ligand-efficient DYRK1A inhibitor. |
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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. |
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V99644 | Dyrk1A-IN-10 | 2891824-14-7 | Dyrk1A-IN-10 (Compound B4) is a DYRK1A inhibitor with antidiabetic activity. |
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V93134 | Dyrk1A-IN-11 | 3058626-26-6 | Dyrk1A-IN-11 (Compound 166) is a potent dual-specific tyrosine phosphorylation regulator 1A (DYRK1A) inhibitor with EC50 of 0.0021 µM. |
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V110390 | Dyrk1A-IN-15 | 1448757-02-5 | Dyrk1A-IN-15 is a selective, blood-brain barrier-crossing ATP-competitive DYRK inhibitor with an IC50 value of 19 nM for Dyrk1A. |
|
V111046 | Dyrk1A-IN-16 | 2805339-74-4 | Dyrk1A-IN-16 is a selective, blood-brain barrier-crossing ATP-competitive DYRK inhibitor with an IC50 value of 53 nM for Dyrk1A. |
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V84259 | Dyrk1A-IN-6 | ||
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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. | |
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V88016 | Dyrk1A-IN-8 | 101578-13-6 | Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A with IC50 of 209 nM. |
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V88018 | Dyrk1A-IN-9 | Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC50: 1.67 μM). | |
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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. |
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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 |
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