DYRK
Dual specificity tyrosine phosphorylation regulated kinase; Dual specificity tyrosine regulated kinase
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. DYRKs contain five members in humans that are clustered into two classes based on their phylogenetic relationships: class I DYRKs, DYRK1A and DYRK1B and class II DYRKs, DYRK2, DYRK3, and DYRK4.
DYRK kinases are “dual specificity” kinases, as they can phosphorylate both tyrosine (Y) and serine/threonine (S/T) residues, although Y-phosphorylation is limited to their autophosphorylation activity. DYRK kinases phosphorylate a broad set of substrates that are involved in a wide range of cellular processes, and they are thought to fulfill essential biological functions both during development and in maintaining homeostasis during the adult life. Consequently, the aberrant regulation or expression of DYRK kinases has been associated with several human pathologies, including cancer.
DYRK Isoform Specific Products
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DYRK Related Products (122)
Related Products (122)
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Antibodies (1)
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DYRK Isoform Comparison
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XRF-1021
0 ImagesCat. No.: HY-179378CAS No.: 2968523-32-0XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.
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UNC9750
0 ImagesCat. No.: HY-175477CAS No.: 2967648-29-7UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC50 values of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP5, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP7 levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma.
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Dyrk1A/α-synuclein-IN-2
0 ImagesCat. No.: HY-144696CAS No.: 2789711-66-4Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect.
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hAChE-IN-8
0 ImagesCat. No.: HY-163514hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.
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Aristolactam A IIIa
0 ImagesCat. No.: HY-N2892CAS No.: 97399-91-2Synonyms: Aristololactam A IIIa; Sch 546909Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells.
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JH-XIV-68-3
0 ImagesCat. No.: HY-144617CAS No.: 2426628-29-5JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines.
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DYRKs-IN-2
0 ImagesCat. No.: HY-128759CAS No.: 1386980-04-6DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.
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Dyrk1A-IN-10
0 ImagesCat. No.: HY-159496CAS No.: 2891824-14-7Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor with antidiabetic activity. Dyrk1A-IN-10 can promote pancreatic β-cell proliferation, increase insulin secretion, and lower blood sugar.
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Dyrk1A-IN-8
0 ImagesCat. No.: HY-158212CAS No.: 101578-13-6Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A , with the IC50 of 209 nM. Dyrk1A-IN-8 plays an important role in neurodegenerative diseases.
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Haspin-IN-1
0 ImagesCat. No.: HY-146586CAS No.: 2768474-30-0Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC50 of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC50s of 221 nM and 916.3 nM, respectively.
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2-Methyl-5-acetylphenol
0 ImagesCat. No.: HY-W152736CAS No.: 33414-49-22-Methyl-5-acetylphenol is a hydroxylated methylacetophenone that exists in the aerial parts of Cannabis sativa subsp. sativa. 2-Methyl-5-acetylphenol exhibits strong binding affinity to HIPK2. 2-Methyl-5-acetylphenol cannot reverse MPP+ (1-methyl-4-phenyl-pyridinium ion)-induced neuronal cytotoxicity. 2-Methyl-5-acetylphenol can be used for Parkinson's disease research.
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DYRK1A Human Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04094DYRK1A Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
