Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PROTAC Aurora-A/Aurora-B Degrader
dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM). It effectively induces the degradation of these kinases, leading to reduced N-Myc levels and decreased viability in IMR32 neuroblastoma cells. dAurAB5 also downregulates AAK1, PTK2, GAK, and TTK, making it a valuable tool for investigating the molecular mechanisms in neuroblastoma and related cancers. -
FAK/Aurora Kinase Inhibitor
FAK/Aurora kinase-IN-1 is a dual inhibitor targeting focal adhesion kinase (FAK) and Aurora kinase, exhibiting IC50 values of 6.61 nM and 0.91 nM, respectively. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and therapeutic development. Its efficacy in inhibiting both kinases positions it as a promising candidate for further studies in tumor proliferation and treatment strategies. -
FLuc Inhibitor
GW694590A is an inhibitor targeting firefly luciferase (Fluc) that enhances the stability of the MYC protein, subsequently increasing its endogenous levels. This compound also inhibits receptor tyrosine kinases, demonstrating significant reductions in DDR2, KIT, and PDGFRα activity at 1 μM. GW694590A serves as a versatile protein kinase inhibitor, influencing both ATP-dependent and -independent luciferase systems, making it valuable for studies in cellular signaling and gene expression regulation. -
Aurora kinase Inhibitor
Aurora kinase-IN-10 is a selective inhibitor of Aurora kinases, demonstrating IC50 values of 5.94 nM for Aurora A and 86.06 nM for Aurora B. This compound exhibits significant anti-tumor activity, making it a valuable tool for research into various cancers, particularly triple-negative breast cancer. Its targeted inhibition of Aurora kinases positions it as a candidate for studies focused on cell cycle regulation and cancer treatment strategies. -
Aurora B inhibitor
Ceftriaxone is a third-generation cephalosporin antibiotic that primarily targets the Aurora B kinase, exhibiting notable inhibitory activity. This compound is also recognized for its broad-spectrum antibacterial efficacy against various Gram-negative and Gram-positive bacteria. Additionally, Ceftriaxone displays anti-inflammatory, antitumor, and antioxidant properties, making it valuable in research applications related to bacterial infections and conditions such as meningitis. -
GRK6/Aurora A Dual Inhibitor
GRK6/Aurora A-IN-1 is a potent dual inhibitor targeting G protein-coupled receptor kinase 6 (GRK6) and Aurora A, exhibiting IC50 values of 120 nM and 11 nM, respectively. GRK6 plays a critical role in the survival of multiple myeloma (MM) cells, making this compound valuable for research in MM studies. This inhibitor can facilitate investigations into the mechanisms of MM cell proliferation and the potential for targeted therapies. -
Aurora A Inhibitor
TAS-119 is a highly selective and orally bioavailable inhibitor of Aurora A with an IC50 of 1.0 nM. It demonstrates significant selectivity for Aurora A compared to other kinases, such as Aurora B, which has an IC50 of 95 nM. TAS-119 exhibits strong antitumor activity, making it a valuable reagent for cancer research focusing on targeted therapies and the exploration of cell cycle regulation. -
Aurora-A/N-Myc Degrader
HLB-0532259 is a PROTAC degrader targeting Aurora-A and N-Myc, designed to selectively induce the degradation of these oncoproteins. In non-MYCN amplified MCF-7 cells, HLB-0532259 shows a degradation concentration (DC50) of 20.2 nM for Aurora-A, while in MYCN amplified SK-N-BE and Kelly cells, it demonstrates DC50 values of 179 nM and 229 nM for N-Myc, respectively. This compound has also exhibited significant antitumor efficacy in mouse models, making it a valuable reagent for cancer research focusing on targeted protein degradation. -
Aurora A Inhibitor
CD532 hydrochloride is a selective inhibitor of Aurora A kinase, exhibiting an IC50 value of 45 nM. This compound not only inhibits Aurora A activity but also promotes the degradation of MYCN. Additionally, CD532 hydrochloride directly interacts with AURKA, leading to a significant conformational change. This reagent is valuable for cancer research, particularly in studies focusing on cell proliferation and tumor progression. -
Aurora Kinase Inhibitor
Aurora kinase inhibitor-2 is a selective, ATP-competitive inhibitor targeting Aurora kinases A and B, exhibiting IC50 values of 310 nM and 240 nM, respectively. This compound is valuable for studying cell cycle regulation and mitosis, making it suitable for research applications related to cancer biology and therapeutic development. Its precision in inhibiting aurora kinase activity allows for further exploration of signaling pathways associated with tumor growth and progression. -
Aurora-A/Aurora-B PROTAC Degrader
dAurAB2 is a dual-targeting PROTAC designed to degrade Aurora-A and Aurora-B, demonstrating potent efficacy with DC50 values of 59 nM and 39 nM, respectively. This compound effectively reduces N-Myc protein levels in MYCN-amplified IMR32 neuroblastoma cells, making it a valuable tool for neuroblastoma research. The unique design incorporates a specific Aurora ligand and an E3 ligase ligand connected by a tailored linker, facilitating targeted degradation and advancing studies in cancer biology. -
Aurora-A Inhibitor
Aurora-A ligand 1 is a specific inhibitor of Aurora-A, exhibiting a high-affinity binding with a dissociation constant (Kd) of 0.85 nM. It serves as a crucial ligand for the development of PROTAC-based Aurora-A degraders, contributing to anti-tumor activity. Additionally, Aurora-A ligand 1 can be utilized in the synthesis of HLB-0532259, which has demonstrated potent anti-tumor effects against neuroblastoma, highlighting its potential in cancer research. -
MASTL/Aurora A Kinase Dual Inhibitor
MASTL/Aurora A-IN-1 is a dual inhibitor of MASTL and Aurora A kinases, exhibiting IC50 values of 0.56 μM and 0.16 μM, respectively. This compound demonstrates broad-spectrum anticancer activity, showing potent effects against various cell lines, including SR, K-562, MDA-MB-435, MOLT-4, and SK-MEL-2, with GI50 values ranging from 0.023 to 0.051 μM. By inhibiting these kinases, MASTL/Aurora A-IN-1 induces G2/M cell cycle arrest, thereby effectively inhibiting cancer cell proliferation. Its application is particularly valuable in cancer research, especially for studying tumors with dysregulated mitosis. -
Aurora Kinase Inhibitor
Aurora Kinase Inhibitor-8 selectively targets Aurora kinases, which play critical roles in mitotic regulation and are frequently implicated in tumorigenesis. This compound exhibits potent inhibitory activity, making it a valuable tool for studying the cell cycle and cancer biology. Research applications include elucidating the mechanisms of cell proliferation and exploring therapeutic strategies for cancer treatment. -
Aurora A kinase Inhibitor
Aurora kinase inhibitor-13 is a selective inhibitor of Aurora A kinase, exhibiting an IC50 value of 2.3 μM. This compound effectively disrupts the function of Aurora A, a key regulator of cell cycle progression. Its ability to modulate Aurora kinase activity makes it valuable for research focused on cancer biology and the development of targeted therapeutics. -
Aurora Kinase A Inhibitor
Aurora kinase-IN-4 is a covalent and ATP-competitive inhibitor of Aurora Kinase A, exhibiting an IC50 of 1.7 nM. This compound demonstrates significant activity in inhibiting cell proliferation across various cancer cell lines, including SJSA-1, MDA-MB-231, A54, and HeLa, with IC50 values of 4.27, 1.54, 3.08, and 6.99 μM, respectively. Aurora kinase-IN-4 is particularly relevant for research into triple-negative breast cancer (TNBC), making it a valuable tool for studies in oncology. -
Aurora A PROTAC Degrader
AurAP14 is a PROTAC degrader specifically targeting Aurora A, with a DC50 of 120 nM. This compound exhibits potent inhibitory effects on various tumor cell lines, showing IC50 values of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis while effectively arresting A549 cells in the S and G2/M phases of the cell cycle. Additionally, AurAP14 demonstrates significant anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR, making it a valuable tool for research focused on treating Aurora A-overexpressing non-small cell lung cancer (NSCLC). -
CDK4/6/9-AURKA/B Inhibitor
LCI133 is a selective multikinase inhibitor targeting CDK4, CDK6, CDK9, and AURKA/B, exhibiting nanomolar potency (IC50 values of 4.7 nM, 10.2 nM, 4.1 nM, 2.8 nM, and 10.6 nM, respectively). It effectively induces S/G2 cell-cycle arrest and promotes significant apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. Additionally, LCI133 demonstrates notable antitumor efficacy in preclinical models, particularly in BE(2)-C neuroblastoma xenograft studies, making it a valuable tool for cancer research and therapeutic development. -
Aurora kinase A/B Inhibitor
IBPR002 is a potent inhibitor of Aurora kinase A and B, exhibiting IC50 values of 41 nM and 17 nM, respectively. This compound disrupts the nucleation and bundling of kinetochore microtubules, impairs the bipolarity of mitotic spindles, and enhances the binding of non-phosphorylated hepatoma up-regulated protein (HURP) to mother centrosome-derived microtubules. IBPR002 demonstrates significant anti-tumor activity in a colorectal cancer xenograft model, making it valuable for research focused on colorectal cancer mechanisms and therapeutics. -
Aurora Kinase Inhibitor
AKI-001 is a potent inhibitor of Aurora kinases, specifically targeting Aurora A and Aurora B with an IC50 of less than 100 nM. This pentacyclic compound demonstrates significant cellular efficacy, making it a valuable tool for investigating cell cycle regulation and mitotic progression. Its selective inhibitory action positions AKI-001 as an essential reagent for research in cancer biology and therapeutic development. -
Aurora A/PKC Inhibitor
(Rac)-Aurora A/PKC-IN-1 is a potent inhibitor of Aurora A and protein kinase C (PKC) isoforms α, β1, β2, and θ. This compound demonstrates significant antiproliferative effects in breast cancer cell lines in vitro and exhibits antimetastatic properties in vivo. It serves as a valuable tool for researchers investigating the role of these kinases in cancer biology and therapeutic strategies. -
BET/Aurora kinase Inhibitor
BET/Aurora kinase-IN-1 is a dual inhibitor targeting both BET and Aurora kinases. This compound demonstrates significant antiproliferative activity across various cancer cell lines and exhibits notable antitumor efficacy in xenograft models of renal cell cancer and colon cancer, achieving tumor growth inhibition rates of 45.99% and 53.06%, respectively. BET/Aurora kinase-IN-1 is a valuable tool for researchers investigating cancer biology and therapeutic strategies targeting these kinases. -
Aurora Kinase Inhibitor
SNS-314 is a potent and selective inhibitor of aurora kinases, demonstrating IC50 values of 9 nM for Aurora A, 31 nM for Aurora B, and 6 nM for Aurora C. This compound effectively disrupts mitotic processes and is valuable in cancer research for studying cell cycle regulation and tumor growth inhibition. SNS-314 is particularly useful for investigations into therapies targeting aurora kinases in various malignancies. -
Aurora A Inhibitor
MLN8054 sodium is a selective inhibitor of Aurora A kinase, which plays a critical role in cell cycle regulation. This compound enhances radiosensitivity and can activate DNA double-strand break responses in prostate cancer cells during in vitro assays. Its mechanism induces accumulation of cells in the G2/M phase and promotes polyploidy. In vivo studies demonstrate that MLN8054 sodium significantly delays tumor growth and enhances apoptosis in cancer cells when administered alongside radiotherapy, making it a valuable tool for cancer research and treatment strategies. -
Aurora B Inhibitor
Aurora kinase inhibitor-10 is a potent inhibitor of Aurora B with an IC50 of 8 nM. This small molecule demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to selectively target Aurora B kinase supports investigations into mitotic regulation and offers potential therapeutic insights for tumor treatments. -
Aurora-A Ligand
Aurora-A ligand 2 is a selective ligand for the Aurora-A kinase, functioning as a crucial component in PROTAC technology. It plays a significant role in the targeted degradation of Aurora-A, facilitating the investigation of its biological implications in cancer research. This compound is valuable for studying Aurora-A kinases and exploring therapeutic strategies in oncology. -
Aurora Kinase Inhibitor
Aurora kinase inhibitor-11 is a potent inhibitor of Aurora Kinase, exhibiting an IC50 of 0.14 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research applications focused on cancer biology and therapeutic strategies targeting mitotic processes. Its efficacy in modulating kinase activity positions it as a relevant candidate for studies aimed at understanding tumorigenesis and developing novel cancer treatments.
