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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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 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 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. -
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 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. -
Aurora Kinase Inhibitor
Tripolin A is a selective non-ATP competitive inhibitor of Aurora A kinase, exhibiting IC50 values of 1.5 μM for Aurora A and 7 μM for Aurora B. This compound plays a crucial role in modulating cell cycle progression by targeting Aurora kinases, making it valuable in cancer research. Tripolin A is used to investigate the mechanisms of mitotic regulation and potential therapeutic strategies in tumor cells. -
Aurora Kinase Inhibitor
XMD-12 is a selective Aurora kinase inhibitor that demonstrates significant anti-tumor activity. It effectively enhances paclitaxel-induced cell death and exhibits high potency against Aurora A, B, and C kinases, with IC50 values of 5.6, 18.4, and 24.6 nM, respectively. This compound is valuable for research applications in cancer biology and therapy development. -
Aurora Kinases Inhibitor
Aurora kinase-IN-2 is a potent inhibitor of Aurora kinases, demonstrating IC50 values of 90 nM for Aurora A and 152 nM for Aurora B. This compound effectively induces cell cycle arrest at the G2/M phase by modulating cyclin B1 and cdc2. It is primarily utilized in cancer research to explore the role of Aurora kinases in tumorigenesis and therapeutic response. -
Aurora A Inhibitor
Aurora A Inhibitor 1 is a potent and selective inhibitor of the Aurora A kinase, which plays a crucial role in regulating cell division and has been implicated in various cancers. Overexpression of Aurora A is associated with oncogenic properties, making it an important target for cancer research. This compound is suitable for studies focusing on the therapeutic modulation of Aurora A in diverse cancer types. -
Aurora Kinase Inhibitor
Aurora kinase inhibitor-9 is a potent dual inhibitor of Aurora A and Aurora B kinases, exhibiting IC50 values of 0.093 µM and 0.09 µM, respectively. This compound demonstrates significant anti-proliferative activity across various cancer cell lines, making it a valuable tool in cancer research. Its ability to target key regulators of cell division positions it as a candidate for studies investigating mitotic disruption and the development of novel cancer therapies. -
Aurora Inhibitor
TAK-901 hydrochloride is a potent inhibitor of aurora kinases A and B, exhibiting IC50 values of 21 nM and 15 nM, respectively. This compound disrupts cell cycle progression, making it a valuable tool in cancer research and therapeutic development. Its ability to inhibit aurora kinases positions TAK-901 hydrochloride as an important reagent for studying mitotic regulation and exploring targeted cancer therapies. -
Aurora Kinase Inhibitor
Tripolin B is an ATP-competitive inhibitor targeting Aurora kinases, exhibiting IC50 values of 2.5 µM and 6 µM for Aurora A and Aurora B kinases, respectively. This compound has demonstrated selectivity in its inhibition profile and is primarily utilized in cellular studies to explore the roles of Aurora kinases in cell cycle regulation and cancer progression. Tripolin B can be a valuable tool in research focused on cell division and oncogenic signaling pathways. -
Aurora Kinase Inhibitor
BI 831266 is a potent and selective inhibitor of Aurora kinase B, a critical regulator of mitosis. This compound exhibits significant antitumor activity, making it valuable for cancer research. Its inhibition of Aurora B can lead to disruptions in cell division, providing insights into potential therapeutic applications for various malignancies. -
Aurora A/B Kinases Inhibitor
TY-011 is a selective inhibitor of Aurora A and B kinases, disrupting normal microtubule-kinetochore attachment. This interference results in DNA damage and apoptosis, effectively inhibiting the proliferation of human gastric cancer cells, with observed IC50 values between 0.11 and 4.49 μM across various gastric cancer cell lines. TY-011 serves as a valuable tool in the study of gastric cancer and the mechanisms underlying mitotic regulation. -
Aurora Kinase Inhibitor
OM137 is a potent Aurora Kinase inhibitor, demonstrating IC50 values of 21.7 μM for Aurora A kinase and 2.4 μM for Aurora B kinase. Additionally, OM137 affects cell cycle regulation by inhibiting Cdk1/cyclinB and Cdk5/p25, also with an approximate IC50 of 20 μM. This compound is notable for its ability to reduce spindle checkpoint-signaling proteins, such as Mad2 and BubR1, at the kinetochores of chromosomes, making it a valuable tool in cancer research and studies on mitotic regulation. -
Aurora Kinase Inhibitor
AT9283 hydrochloride is a multi-targeted kinase inhibitor that primarily targets Aurora A and Aurora B kinases, which play critical roles in cell proliferation and survival. Its inhibitory effects extend to additional kinases such as JAK2 and Abl (T315I), enhancing its potential utility in cancer research. AT9283 hydrochloride has demonstrated significant anti-tumor activity, making it a valuable tool for investigating therapeutic strategies in various malignancies. -
Aurora Kinase Inhibitor
VE-465 is a potent Aurora kinase inhibitor that promotes apoptosis in cancer cells. Its anticancer activities have been demonstrated across various tumor models, making it a valuable tool for cancer research. This compound's ability to selectively target Aurora kinases positions it as a significant candidate for investigations into tumor progression and treatment strategies.
