DYRK1
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) is a serine/threonine kinase that regulates neuronal differentiation, synaptic plasticity, and cell cycle progression[1][4]. Mechanistically, DYRK1A modulates pre- and post-synaptic signaling and alternative splicing, thereby influencing neuronal development and adult cognitive function[3][1]. DYRK1A activity affects cytoskeletal dynamics through MKL1-mediated pathways, promoting morphogenesis in human neonatal megakaryocytes[2]. Overexpression or dosage imbalance of DYRK1A contributes to neurodevelopmental disorders such as Down syndrome and MRD7, and to neurodegenerative diseases including Alzheimer’s and Parkinson’s disease[1][4][5]. Compared with related isoforms DYRK1B and DYRK2, DYRK1A uniquely regulates central nervous system processes, including tau phosphorylation and APP processing, while DYRK1B predominantly modulates stem cell behavior and metabolic pathways[1][6][7]. Pharmacologically, small molecule inhibitors such as harmine, AnnH75, and thiazoloquinazolines selectively target DYRK1A, enabling modulation of neuronal differentiation, alternative splicing, and pathological tau phosphorylation, with minimal off-target activity[3][4][6][8]. Agonists and inhibitors of DYRK1A also facilitate experimental studies of megakaryocyte morphogenesis, bipolar androgen therapy in prostate cancer, and CNS-related cellular senescence[2][9]. Structural studies reveal that inhibitor binding exploits ATP-competitive mechanisms and hinge region interactions, supporting development of isoform-selective chemical probes for translational research[8].
References:
- [1]. Arbones ML, et al. DYRK1A and cognition: A lifelong relationship. Pharmacol Ther. 2019 Feb;194:199-221. [Content Brief]
- [2]. Elagib KE, et al. Relieving DYRK1A repression of MKL1 confers an adult-like phenotype to human infantile megakaryocytes. J Clin Invest. 2022 Oct 3;132(19):e154839. [Content Brief]
- [3]. Rüben K, et al. Selectivity Profiling and Biological Activity of Novel β-Carbolines as Potent and Selective DYRK1 Kinase Inhibitors. PLoS One. 2015 Jul 20;10(7):e0132453. [Content Brief]
- [4]. Kargbo RB. Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, et al. Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome. ACS Med Chem Lett. 2020 Jul 9;11(10):1795-1796. [Content Brief]
- [5]. Demuro S, et al. GSK-3β, FYN, and DYRK1A: Master Regulators in Neurodegenerative Pathways. Int J Mol Sci. 2021 Aug 23;22(16):9098. [Content Brief]
- [6]. Foucourt A, et al. Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II. Molecules. 2014 Sep 26;19(10):15411-39. [Content Brief]
- [7]. Kokkorakis N, et al. Minibrain-related kinase/dual-specificity tyrosine-regulated kinase 1B implication in stem/cancer stem cells biology. World J Stem Cells. 2020 Dec 26;12(12):1553-1575. [Content Brief]
- [8]. Kaltheuner IH, et al. Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. Nat Commun. 2021 Nov 16;12(1):6607. [Content Brief]
- [9]. Atri Roozbahani G, et al. Induction of cellular senescence by androgen receptor agonist or antagonist is mediated via two novel common DYRK1A-DREAM and cyclin G2 signaling pathways in castration-resistant prostate cancer. J Adv Res. 2026 Feb;80:371-392. [Content Brief]
All Product Categories
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DYRK1 Related Products (64)
Related Products (64)
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VS-II-173
0 ImagesCat. No.: HY-122670CAS No.: 1627962-21-3VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
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JH-XVII-10
0 ImagesCat. No.: HY-144614CAS No.: 3034312-17-6JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.
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GSK3-IN-10
0 ImagesCat. No.: HY-172198CAS No.: 844441-56-1GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC50 of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress.
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Dyrk1A-IN-15
0 ImagesCat. No.: HY-179599CAS No.: 1448757-02-5Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research.
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Dyrk1A/α-synuclein-IN-1
0 ImagesCat. No.: HY-144695CAS No.: 2789711-47-1Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect.
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Dyrk1A-IN-16
0 ImagesCat. No.: HY-179600CAS No.: 2805339-74-4Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research.
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Dyrk1A-IN-1
0 ImagesCat. No.: HY-139830CAS No.: 2858696-72-5Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
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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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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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KTD-092
0 ImagesCat. No.: HY-173615KTD-092 is a hit for DYRK1A inhibition, with an IC50 of 22 nM for human DYRK1A. KTD-092 can be used in the research for Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes and other neurodegenerative diseases.
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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.: 2768474-30-0
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GNF7156
0 ImagesCat. No.: HY-183955CAS No.: 2041071-54-7GNF7156 is a DYRK1A/GSK3B inhibitor, IC50 values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes.
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Multi-kinase-IN-14
0 ImagesCat. No.: HY-181046CAS No.: 2201083-51-2Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.
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Licocoumarone
0 ImagesCat. No.: HY-N20713CAS No.: 118524-14-4Licocoumarone is an active component derived from licorice. Licocoumarone has an IC50 of 12.56 μM and a Kd of 14.90 μM against human DYRK1A. Licocoumarone inhibits NF-κB activation by blocking IκBα degradation and p65 phosphorylation, interferes with MAPK activation via inhibiting phosphorylation, and downregulates the expression of iNOS. Licocoumarone inhibits LPS-induced expression of IL-1β, IL-6 and IL-10; it induces apoptosis of pancreatic cancer cells apoptosis and acts as a neuraminidase inhibitor (IC50 = 27.8 μM). Licocoumarone exhibits anti-inflammatory and antimicrobial activities, with antibacterial activity against Listeria and antifungal activity against Candida parapsilosis. Licocoumarone can be used in studies related to immune and inflammatory diseases, pancreatic cancer, and specific bacterial and fungal infections.
