Catalog No.
Product Name
Application
Product Information
Citations
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DYRK1A Inhibitor
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. -
DYRK1A Inhibitor
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. -
DYRK1A/GSK3β Inhibitor
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. -
Dyrk1A And Dyrk1B Inhibitor
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. -
DYRK1A Inhibitor
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. -
DYRK Inhibitor
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. -
Dyrk1B Kinase Inhibitor
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/DYRK2 Inhibitor
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 Inhibitor
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. -
DYRK2 Inhibitor
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 Inhibitor
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. -
Casein Kinase/DYRK/TNIK Inhibitor
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. -
DYRK1A Inhibitor
7-Deazaguanine is a selective inhibitor of DYRK1A, a kinase implicated in various neurological disorders and cancer. This compound demonstrates good blood-brain barrier penetration, making it suitable for studies related to Down's syndrome and oncogenic processes. Its unique properties facilitate research into the therapeutic potential of targeting DYRK1A in these contexts. -
DYRK/CLK Inhibitor
Leucettinib-92 is a selective inhibitor of DYRK and CLK kinases, demonstrating IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, and 124 nM for DYRK1A, among others. This compound exhibits significant biological activity by modulating kinase signaling pathways, making it a valuable tool for research in oncology and neurodegenerative diseases. Its potency against key kinases provides potential insights into therapeutic targeting and intervention strategies in various cellular processes. -
DYRK1A/1B Inhibitor
EHT 5372 is a potent and selective inhibitor of the DYRK family of kinases, demonstrating IC50 values of 0.22 nM for DYRK1A and 0.28 nM for DYRK1B. It exhibits notable inhibition against other members of the DYRK family and related kinases, making it a valuable tool for investigating the role of DYRKs in cellular signaling pathways. EHT 5372 is primarily utilized in research applications focused on neurodegenerative diseases and cancer, facilitating studies on cell proliferation, differentiation, and apoptosis. -
DYRK1A Inhibitor
GNF2133 hydrochloride is a selective and orally active inhibitor of DYRK1A, exhibiting an IC50 of 0.0062 µM for DYRK1A while remaining inactive against GSK3β at concentrations exceeding 50 µM. This compound demonstrates significant efficacy in enhancing proliferation and functioning of both rat and human primary β-cells. Additionally, GNF2133 hydrochloride enhances glucose disposal and promotes insulin secretion, making it a valuable tool for research in type 1 diabetes. -
DYRKs Inhibitor
DYRKs-IN-1 hydrochloride is a selective inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), showing IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B. This compound exhibits antitumor activity, making it a valuable tool for cancer research. Its ability to modulate kinase activity positions it as a significant reagent for studying the role of DYRKs in oncogenesis and therapeutic interventions. -
DYRK1A Inhibitor
RD0392 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) with an IC50 of 1.3 nM. It exhibits significant potential in the study of neurodegenerative diseases, particularly Alzheimer's disease, by modulating pathways involved in neuroprotection and neuronal function. This compound is a valuable tool for researchers exploring the therapeutic implications of DYRK1A inhibition in neurodegenerative conditions. -
CDK/DYRK Inhibitor
ML 315 hydrochloride is a selective dual inhibitor targeting cyclin-dependent kinases (CDKs) and dual-specificity tyrosine-regulated kinases (DYRKs), exhibiting IC50 values of 68 nM and 282 nM, respectively. This compound is utilized in research focused on cancer and neurological diseases, providing insights into cell cycle regulation and neurodegenerative pathways. ML 315's potent inhibitory action makes it a valuable tool for studying therapeutic strategies in these critical areas. -
DYRK Inhibitor
Protein Kinase Inhibitor 1 is a selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), demonstrating an IC50 of 74 nM and a Kd of 9.5 nM. This compound is instrumental in the investigation of DYRK1A's role in various cellular processes, including neurodevelopment and cancer progression. It serves as a valuable tool for research applications focused on kinase signaling pathways and their implications in disease states. -
CDK Inhibitor
(R)-(+)-O-Demethylbuchenavianine is a selective inhibitor of Cyclin-dependent kinases (CDKs), specifically targeting CDK1 and CDK5 with IC50 values of 1.1 and 0.95 μM, respectively. Additionally, it shows inhibitory activity against glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1), and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), though with IC50 values greater than 10 μM. This compound is important for research focused on cell cycle regulation, cancer therapeutics, and neurodegenerative diseases. -
CDK/DYRK Inhibitor
ML 315 is a selective dual inhibitor of cyclin-dependent kinases (CDK) and dual-specificity tyrosine phosphorylation-regulated kinase (DYRK), exhibiting IC50 values of 68 nM and 282 nM, respectively. It demonstrates significant biological activity in modulating cell cycle progression and neuronal signaling pathways. This compound has applications in cancer research and the study of neurological diseases, facilitating insights into therapeutic targets within these areas. -
DYRKs Inhibitor
DYRKs-IN-1 is a potent inhibitor of dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), effectively targeting DYRK1A and DYRK1B with IC50 values of 5 nM and 8 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for research in cancer biology and potential therapeutic applications. Its specificity and efficacy support further investigations into the role of DYRKs in cell signaling and tumor progression. -
DYRK1A/DYRK1B Inhibitor
Dyrk1A/B-IN-1 is a selective inhibitor targeting DYRK1A and DYRK1B, exhibiting Kis of 67.8 nM and 237.9 nM, and IC50s of 1.1 μM and 0.8 μM, respectively. This compound is cell-permeable and non-toxic to human cells, making it suitable for investigating the cellular functions of DYRK1A and DYRK1B. Dyrk1A/B-IN-1 is valuable for research applications focused on understanding the role of these kinases in various pathological conditions. -
DYRK Inhibitor
TSL2109 is a selective DYRK2 and CDK4/6 inhibitor, exhibiting an IC50 of 22 nM for DYRK2. This compound induces cell cycle arrest and apoptosis in vitro, effectively suppressing tumor growth in the context of Enzalutamide resistance. TSL2109 demonstrates a safety profile suitable for research applications in prostate and breast cancer studies, highlighting its potential as a therapeutic agent in oncology. -
DYRK2 Inhibitor
DYRK2-IN-2 is a selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2), exhibiting an IC50 of 40.3 nM. This compound demonstrates low inhibitory activity against other DYRK family members and CDC-like kinases, making it a specific tool for studying DYRK2. DYRK2-IN-2 effectively inhibits tau protein phosphorylation at Thr212 and exhibits moderate cytotoxicity in HT22 neuronal cells. This reagent is valuable for investigating the role of DYRK2 in cancer biology and neurodegenerative diseases. -
Dyrk1A/α-syn Inhibitor
Dyrk1A/α-synuclein-IN-1 is an inhibitor targeting both Dyrk1A and α-synuclein aggregation, demonstrating IC50 values of 177 nM and 10.5 µM, respectively. This dual-action compound is noted for its potential neuroprotective effects and favorable central nervous system penetration. It is applicable in research surrounding neurodegenerative diseases and the modulation of protein aggregation pathways. -
DYRK Inhibitor
Dyrk1A-IN-1 is a selective inhibitor of Dyrk1A kinase activity, demonstrating an IC50 of 119 nM. This compound effectively inhibits the aggregation of tau and α-synuclein oligomers, making it a valuable tool for investigating neurodegenerative diseases. Its capacity to modulate kinase activity and prevent protein aggregation highlights its potential in studying pathways associated with tauopathies and synucleinopathies. -
DYRK Kinases Substrate
Woodtide is a specific substrate for the DYRK family of kinases, derived from the phosphorylation site sequence of FKHR. This reagent is utilized in biochemical assays to investigate DYRK kinase activity and regulation, facilitating studies on cellular signaling pathways and developmental processes. Its application is crucial for researchers exploring the roles of DYRK kinases in various biological contexts, including cancer and neurodegenerative diseases. -
Dyrk1A/α-syn Inhibitor
Dyrk1A/α-synuclein-IN-2 is an effective inhibitor targeting both Dyrk1A and α-synuclein aggregation, with an IC50 value of 7.8 µM for α-synuclein. This compound demonstrates significant potential for central nervous system (CNS) penetration and exhibits neuroprotective properties. It is particularly useful in research focused on neurodegenerative diseases and understanding the molecular mechanisms underlying α-synuclein pathology. -
DYRK1A Inhibitor
Aristolactam A IIIa functions as a DYRK1A inhibitor and is derived from the alkaloid structure found in Glycosmis chlorosperma. This compound demonstrates significant inhibition of platelet aggregation induced by arachidonic acid, collagen, and platelet-activating factor. Additionally, Aristolactam A IIIa exhibits potent cytotoxic effects on HeLa cells, making it a valuable tool for research in cancer biology and cellular signaling pathways. -
DYRK1A/B Inhibitor
JH-XIV-68-3 is a selective inhibitor of DYRK1A and DYRK1B, targeting these kinases to modulate downstream signaling pathways. This compound exhibits significant antitumor activity in head and neck squamous cell carcinoma (HNSCC) cell lines, making it a valuable tool for cancer research. Its specificity for DYRK1A and DYRK1B is confirmed through biochemical and cellular assays, supporting its potential in therapeutic applications targeting these kinases. -
DYRK Inhibitor
DYRKs-IN-2 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family members, exhibiting IC50 values of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its selective inhibition of DYRKs enables exploration of their roles in cellular signaling pathways and therapeutic potential in oncology. -
Dyrk1A Inhibitor
AnnH31 is a selective inhibitor of Dyrk1A with an IC50 value of 81 nM. In addition, AnnH31 inhibits monoamine oxidase A (MAO-A) at an IC50 of 3.2 μM. This compound has been shown to reduce cell viability in HeLa, PC12, and SH-SY5Y cell lines, making it a valuable tool for research focused on neurodegeneration and cancer biology. -
DYRK1A Inhibitor
Dyrk1A-IN-10 is a potent DYRK1A inhibitor that exhibits antidiabetic activity. It has been shown to promote pancreatic β-cell proliferation and enhance insulin secretion, resulting in reduced blood glucose levels. This compound holds potential for research applications in diabetes treatment and metabolic disorder studies. -
Dyrk1A Inhibitor
Dyrk1A-IN-8 is a specific inhibitor of Dyrk1A, exhibiting an IC50 of 209 nM. This compound is significant for its potential applications in the study of neurodegenerative diseases by modulating kinase activity. Research involving Dyrk1A-IN-8 can provide insights into therapeutic strategies for conditions associated with dysregulated kinase signaling. -
DYRK1A Inhibitor
FINDY is a selective inhibitor of DYRK1A, specifically targeting its folding intermediate. It effectively inhibits autophosphorylation at Ser97, with an IC50 of 35 μM. FINDY is valuable for research on neurological disorders. Additionally, it features an alkyne group that allows it to engage in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool in chemical biology applications. -
MAO-A/DYRK1A Inhibitor
Norharmine is a Harmine analogue that functions as an inhibitor of monoamine oxidase A (MAO-A) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A). It exhibits weak inhibitory activity against MAO-A and demonstrates certain inhibitory effects on DYRK1A, positioning it as a valuable tool for research in neurobiology and cellular signaling pathways. Norharmine is useful in studies focusing on mood disorders and cognitive functions related to these kinase targets. -
DYRK1A Inhibitor
Dyrk1A-IN-11 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), exhibiting an EC50 of 0.0021 µM. This compound effectively inhibits the phosphorylation of Tau at threonine 212, with an EC50 value of 0.0361 µM. Dyrk1A-IN-11 is relevant for research into neurodegenerative diseases and the role of tau phosphorylation in cellular processes. -
DYRK1A Inhibitor
Aristolactam BIII is a selective inhibitor of DYRK1A, demonstrating potent inhibition of the kinase's activity in vitro with an IC50 of 9.67 nM. This compound effectively rescues proliferative defects in DYRK1A transgenic mouse-derived fibroblasts and ameliorates neurological and phenotypic abnormalities in Down syndrome-like Drosophila models. Its applications are valuable in studying the role of DYRK1A in various biological processes and diseases, particularly in the context of developmental disorders. -
DYRK1/DYRK1B Inhibitor
DYRKi is a selective inhibitor of DYRK1 and DYRK1B, exhibiting IC50 values of 3.7 µM and 90 nM, respectively. This compound effectively antagonizes Hh/Gli signaling pathways, disrupting both SMO-dependent and SMO-independent oncogenic GLI activity in human medulloblastoma cells. DYRKi holds potential for research focused on HH/GLI-associated cancers, providing a valuable tool for elucidating the role of these pathways in tumorigenesis. -
DYRK1A/B Inhibitor
ProINDY is a prodrug of INDY that functions as an inhibitor of DYRK1A and DYRK1B. This compound has demonstrated the ability to recover Xenopus embryos from head malformations caused by the overexpression of Dyrk1A. ProINDY is valuable for research applications related to developmental biology and the study of kinase pathways involved in embryogenesis. -
DYRK1A Inhibitor
Dyrk1A-IN-2 is a potent DYRK1A inhibitor with an EC50 of 37 nM. This compound demonstrates significant capacity to promote human β-cell replication while exhibiting low cytotoxicity. Dyrk1A-IN-2 is a valuable tool for research in diabetes and regenerative medicine, aiding in the investigation of β-cell proliferation and function. -
Dyrk1A Inhibitor
Dyrk1A-IN-12 is a selective inhibitor of Dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1A), demonstrating an IC50 of 95 nM. This compound exhibits significant anti-Enterovirus A71 (EV-A71) activity, with an EC50 of 4.4 μM and a cytotoxicity CC50 of 12.8 μM, resulting in a selectivity index of 2.9. Additionally, Dyrk1A-IN-12 shows strong inhibitory effects against herpes simplex virus (HSV), positioning it as a valuable tool for research in viral infections and Dyrk1A-related pathways. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a dissociation constant (KD) of 203 pM. This compound effectively disrupts the function of the KRas signaling pathway, making it a valuable tool for investigating tumor biology and related therapeutic strategies. Deltasonamide 1 holds promise for advancing research in cancer treatment and understanding related pathophysiological mechanisms. -
KRAS Inhibitor
Deltarasin hydrochloride is a potent inhibitor of the interaction between KRAS and PDEδ, exhibiting a binding affinity (Kd) of 38 nM for purified PDEδ. This compound is crucial for research applications focused on targeting KRAS-driven oncogenesis, primarily in cancer studies. By disrupting this interaction, Deltarasin hydrochloride facilitates investigations into therapeutic strategies aimed at KRAS mutations and their downstream signaling pathways. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 TFA is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a binding affinity with a KD of 203 pM. This compound is valuable in research focused on cancer biology, particularly in the study of tumor progression and metastasis. Its ability to disrupt the PDE6δ-KRas axis makes it a useful tool for investigating the underlying mechanisms of KRas-driven malignancies. -
PLK1/p38γ Inhibitor
PLK1/p38γ-IN-1 is a multitarget inhibitor that selectively targets PLK1 and p38γ kinases. This compound has demonstrated the ability to inhibit cell proliferation in human hepatocellular carcinoma and hepatoblastoma cell lines in vitro. PLK1/p38γ-IN-1 is valuable for research focused on cancer biology and the modulation of cell cycle pathways. -
KRAS G12C Inhibitor
KRAS G12C-IN-78 is a selective inhibitor targeting the KRAS G12C mutant protein, binding to both inactive and active states. This compound effectively inhibits ERK1/2 phosphorylation and promotes covalent adduct formation with endogenous KRAS G12C, leading to the suppression of MAPK pathway gene expression and reduced cellular proliferation in KRAS G12C mutant cells. KRAS G12C-IN-78 is suitable for studying KRAS G12C mutant solid tumors, such as pancreatic ductal adenocarcinoma and non-small cell lung cancer. -
Akt/ROCK Inhibitor
Akt/ROCK-IN-1 is a potent dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. This compound demonstrates significant antitumor activity, particularly in neuroblastoma models. It serves as a valuable tool for research into cancer biology and therapeutic development.
