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 (127)
Related Products (127)
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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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PROTAC DYRK2 degrader-2
0 ImagesPROTAC DYRK2 degrader-2 is a PROTAC DYRK2 degrader based on curcumin analog A3. It recruits the CRBN E3 ligase to mediate DYRK2 ubiquitination and achieves degradation via the ubiquitin-proteasome system. PROTAC DYRK2 degrader-2 downregulates the expression level of DYRK2 protein in cancer cells. It is applicable to cancer-related research.
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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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DYRK2 ligand 2
0 ImagesCat. No.: HY-186288CAS No.: 3061366-78-4
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HIPK2-IN-2
0 ImagesCat. No.: HY-189141HIPK2-IN-2 is an orally active and selective HIPK2 inhibitor with an IC50 of 0.36 μM against HIPK2. HIPK2-IN-2 reduces HIPK2 protein expression levels. HIPK2-IN-2 inhibits the proliferation and migration of renal interstitial fibroblasts, alleviates renal tubular injury and collagen deposition, and suppresses TGF-β/Smad3-mediated profibrotic signaling pathways as well as TNF-α/NF-κB-mediated inflammatory signaling pathways in renal cells. HIPK2-IN-2 is used for the study of chronic kidney disease-associated renal fibrosis.
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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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HIPK2-IN-1
0 ImagesCat. No.: HY-189140HIPK2-IN-1 is an orally active and selective HIPK2 inhibitor with an IC50 of 0.56 μM. HIPK2-IN-1 exerts antifibrotic and anti-inflammatory activities. HIPK2-IN-1 binds to HIPK2, inhibits the downstream TGF‑β/Smad3, p53, and TNF‑α/NF‑κB signaling pathways, reduces the expression of fibrotic markers, suppresses cell proliferation and migration, and alleviates renal tubular injury and collagen deposition. HIPK2-IN-1 is used for the study of renal fibrosis associated with chronic kidney disease.
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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.: 1386980-04-6
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Dyrk1A-IN-10
0 ImagesCat. No.: HY-159496CAS No.: 2891824-14-7
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BI-5521
0 ImagesCat. No.: HY-171881CAS No.: 864686-48-6BI-5521 is an orally active GSK-3 inhibitor with an IC50 of 1.1 nM against GSK-3β. BI-5521 targets the two GSK-3 isoforms with similar potency and exhibits potent inhibitory activity against DYRK1A. By modulating GSK-3 activity, BI-5521 inhibits tumor proliferation and cancer cell growth, exerts cytotoxic effects, and reduces cancer cell viability. It shows consistent chemosensitivity across all subtypes of rhabdomyosarcoma, produces synergistic growth inhibitory effects when combined with SOS1 inhibitors, reduces oral glucose levels, regulates the myofibroblast differentiation pathway, decreases the nuclear localization of YAP/SMAD2/3, and lowers the positive rate of α-SMA in fibroblasts without affecting the apoptosis of CD4+ T cells. BI-5521 can be used in the research of non-small cell lung cancer, pleomorphic rhabdomyosarcoma, type 2 diabetes, pancreatic ductal adenocarcinoma, Alzheimer's disease, bipolar disorder, and metabolic dysfunction-associated steatotic liver disease.
