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DYRK inhibitors act on dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) in cell growth. The first family member, Dyrk, was described in 1996 as a kinase whose activity depends on tyrosine residues in its activation loop. DYRK1A lies in the Down syndrome critical region of chromosome 21, and DYRK1B is studied in cell quiescence. The beta-carboline alkaloid harmine inhibits DYRK1A, as shown in a 2007 kinase selectivity screen. AZ191 preferentially inhibits DYRK1B, LDN-192960 targets DYRK2, and GSK-626616 is listed as a DYRK3 inhibitor. The set also contains inhibitors of related targets such as homeodomain-interacting protein kinase 2 (HIPK2) and mitotic kinesin-like protein 2 (MKLP-2).
EHT 1610 is a highly potent and selective inhibitor of dual-specificity tyrosine-phosphorylation-regulated kinases (DYRK), exhibiting IC₅₀ values of 0.36 nM for DYRK1A and 0.59 nM for DYRK1B. EHT 1610 demonstrates significant antileukemic activity, associated with modulation of cell cycle progression and induction of apoptotic pathways in target cells.
ID-8 is a DYRK inhibitor. ID 8 also stimulates proliferation at a steady rate (observed in serum-free media supplemented with 10 μM over a 30 day period).
AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2.
Synonyms: Dyrk1B/A-IN-1; Mirk-IN-1
Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of ?0.33 µM.
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM).
Synonyms: LDN 192960
LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
Dyrk1A-IN-16 is a selective DYRK1A inhibitor that operates as an ATP-competitive antagonist with an IC50 of 53 nM. This compound exhibits strong selectivity for DYRK kinases and demonstrates nanomolar potency in biological assays. In vitro studies reveal that Dyrk1A-IN-16 effectively impairs neurosphere self-renewal, cell invasion, and EGFR stability. In vivo, it has been shown to inhibit tumor growth and extend survival, indicating its potential utility in glioblastoma research.
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Dyrk1A-IN-15 is a selective, ATP-competitive inhibitor of DYRK1A with an IC50 of 19 nM. This compound demonstrates high selectivity for DYRK kinases and nanomolar potency across various kinase assays. In vitro studies reveal that Dyrk1A-IN-15 disrupts neurosphere self-renewal, inhibits cell invasion, and destabilizes EGFR. Additionally, it shows the ability to inhibit tumor growth and extend survival in vivo, indicating its potential utility in glioblastoma research.
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Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). This compound also modulates GSK-3 signaling, demonstrating significant effects on cellular processes by inhibiting apoptosis and reducing reactive oxygen species (ROS) production. Leucettine L41 promotes cell cycle progression and proliferation in β-cells, enhancing insulin secretion. It is a valuable tool for research focused on neurological disorders, including Alzheimer’s disease, and metabolic diseases such as diabetes.
JH-XVII-10 is a highly selective inhibitor of DYRK1A and DYRK1B, exhibiting IC50 values of 3 nM and 5 nM, respectively. This compound demonstrates significant antitumor activity in head and neck squamous cell carcinoma (HNSCC) cell lines. JH-XVII-10 is suitable for research applications focusing on dysregulation of DYRK kinases in cancer.
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GNF2133 is a potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 0.0062 µM for DYRK1A, with minimal activity against GSK3β (>50 µM). This compound has demonstrated significant proliferation potency and efficacy in both rat and human primary β-cells. GNF2133 notably enhances glucose disposal capacity and stimulates insulin secretion, making it a valuable reagent for research into type 1 diabetes.
AO-365/43472821 is a selective inhibitor of Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), with an IC50 of 0.29 μM, and demonstrates potent inhibition of CLK1 (IC50 = 0.08 μM). This compound has been shown to protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid-induced cytotoxicity. Furthermore, AO-365/43472821 effectively reduces the expression levels of phosphorylated tau (pSer396) and Aβ1-42 proteins, making it a valuable reagent for research related to Alzheimer’s disease.
Atalaphyllidine is a selective inhibitor of DYRK1A kinase, demonstrating an IC50 of 2.2 μM. This natural product, derived from the stem bark of Glycosmis chlorosperma, plays a significant role in regulating protein phosphorylation, making it valuable in studies related to neurodegenerative diseases. Its specific mechanism of action positions Atalaphyllidine as a useful tool in understanding the pharmacological modulation of DYRK1A and its implications in various cellular processes.
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GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways.
INDY is a potent Dyrk1A and Dyrk1B inhibitor, acting as an ATP-competitive antagonist with IC50 values of 0.24 μM and 0.23 μM, respectively. By binding to the ATP pocket of these kinases, INDY exhibits a Ki of 0.18 μM for Dyrk1A. This compound significantly diminishes the self-renewal capacity of both normal and tumorigenic cells, making it a valuable tool for research in glioblastoma and neural progenitor cell studies.
DYRK1-IN-1 is a selective inhibitor of the DYRK1A kinase, exhibiting an IC50 value of 220 nM for its phosphorylation activity. It serves as a valuable chemical probe for investigating DYRK1A's role in the central nervous system. This compound is suitable for research applications focused on neurological disorders and the modulation of kinase-mediated signaling pathways.
Protein Kinase Inhibitor 1 Hydrochloride is a selective inhibitor targeting dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). It demonstrates potent inhibition with IC50 values of 136 nM for HIPK1 and 74 nM for HIPK2, alongside a Kd of 9.5 nM for HIPK2. This compound is suitable for studies exploring the role of HIPK family kinases in various signaling pathways and disease models, particularly in cancer research and cellular response to stress.
AZ-Dyrk1B-33 is a potent and selective DYRK1B kinase inhibitor, exhibiting an IC50 of 7 nM. This compound effectively modulates DYRK1B activity, making it a valuable tool for investigating its role in cellular processes. AZ-Dyrk1B-33 is applicable in studies related to neurodegenerative diseases and cancer research, where DYRK1B activity is implicated.
Dyrk1A-IN-4 is a selective DYRK1A and DYRK2 inhibitor, known for its potent activity with IC50 values of 2 nM and 6 nM, respectively. This compound effectively inhibits DYRK1A autophosphorylation at pSer520 in U2OS cells, displaying an IC50 of 28 nM. Dyrk1A-IN-4 is useful for investigating the roles of DYRK1A in various cancer types, including ovarian adenocarcinoma, neuroblastoma, and cervical squamous cell carcinoma.
Dyrk1A-IN-5 is a potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 6 nM. It demonstrates notable selectivity for DYRK1B and CLK1, with IC50 values of 600 nM and 500 nM, respectively, while showing minimal activity against DYRK2 (IC50 > 10 μM). This compound is particularly valuable for research related to Down syndrome, facilitating the exploration of DYRK1A's role in cellular mechanisms associated with this condition.
YK-2-69 is a potent and selective inhibitor of DYRK2, exhibiting an IC50 value of 9 nM. It specifically targets Lys-231 and Lys-234 within the DYRK2 protein, making it a valuable tool for investigating the role of DYRK2 in cellular processes. This compound is primarily utilized in research focused on prostate cancer, providing insights into tumor biology and potential therapeutic strategies.
Dyrk1A-IN-3 is a selective inhibitor of the dual-specificity tyrosine-regulated kinase 1A (DYRK1A), exhibiting a binding affinity with an IC50 of 76 nM. This compound is valuable for investigations into neurodegenerative disorders, including Alzheimer's Disease, Huntington's Disease, and Parkinson's Disease. Researchers can utilize Dyrk1A-IN-3 to explore the role of DYRK1A in neuronal signaling and disease pathology.
ON 108600 is a potent inhibitor of casein kinase 2 (CK2), TYRK1 (DYRK), and TNIK, demonstrating IC50 values of 0.016 μM against DYRK1A, 0.007 μM against DYRK2, 0.05 μM against CK2α1, 0.005 μM against CK2α2, and 0.005 μM against TNIK. This compound exhibits promising antitumor activity, making it a valuable tool for research applications focused on cancer biology, signaling pathways, and kinase inhibition studies. Its specificity for these kinases positions ON 108600 as a critical reagent for investigating therapeutic strategies targeting kinase-related diseases.
