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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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. |
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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). |
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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. |
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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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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. |
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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. |
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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. |
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V69713 | FINDY | 1507367-37-4 | FINDY is an intermediate-fold selective inhibitor of DYRK1A. |
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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. |
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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. |
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V22069 | Harmine | 442-51-3 | Harmine (telepathine) is a naturally occuring beta-carboline and fluorescent harmala alkaloid found in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (formerly known as 'yage' or 'ayahuasca'). |
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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. |
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V69718 | JH-XIV-68-3 | 2426628-29-5 | JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. |
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V52015 | LDN-209929 dihydrochloride | 1784281-97-5 | LDN-209929 di-HCl is a potent and specific inhibitor of haspin kinase (IC50=55 nM), with 180-fold selectivity over DYRK2 (IC50=9.9 μM). |
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V69704 | Protein kinase inhibitor 1 hydrochloride | 2321337-71-5 | Protein kinase inhibitor 1 HCl is a potent HIPK2 inhibitor (antagonist) with IC50s of 136 and 74 nM for HIPK1 and HIPK2 respectively, and a Kd of 9.5 nM for HIPK2. |
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V69709 | Woodtide | 634592-23-7 | Woodtide is a substrate of the DYRK (DYRK) family of kinases and its sequence is based on the sequence surrounding the DYRK phosphorylation site in FKHR. |
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