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Aurora kinase inhibitors block Aurora A, Aurora B and Aurora C, three serine/threonine kinases that coordinate mitosis. The founding aurora gene was described in Drosophila in 1995, where its mutations prevented centrosome separation and produced monopolar spindles. In human cells Aurora A acts at centrosomes and spindle poles during spindle assembly. Aurora B belongs to the chromosomal passenger complex, which moves from centromeres to the spindle midzone during division. Alisertib preferentially inhibits Aurora A, whereas barasertib-HQPA and hesperadin mainly target Aurora B. Work with hesperadin in 2003 linked Aurora B to correcting kinetochore-microtubule attachments and maintaining the spindle assembly checkpoint. Tozasertib and AMG 900 inhibit all three family members and are used as pan-Aurora tools.
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.
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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.
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.
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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.
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.
(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-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.
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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.
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 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-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.
Synonyms: (E)-Tripolin A
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.
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 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 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-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.
BRD-7880 is a potent inhibitor of Aurora Kinase B (AURKB) and Aurora Kinase C (AURKC), demonstrating IC50 values of 7 nM and 12 nM, respectively. This compound exhibits significant selective inhibition, making it a valuable tool in cancer research, particularly in studying the role of these kinases in cell division and tumorigenesis. BRD-7880 may be used to investigate the therapeutic potential of targeting the AURKB/C pathway in various malignancies.
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.
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.
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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.
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.
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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.
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.
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.
Binucleine 2 is an ATP-competitive inhibitor targeting Drosophila Aurora B kinase, displaying an inhibition constant (Ki) of 0.36 μM. This compound exhibits isoform specificity, effectively inhibiting Drosophila Aurora B in a dose-dependent manner while exhibiting minimal activity against human and Xenopus laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 is valuable for studying mitotic processes, as it induces defects in mitosis and cytokinesis in Drosophila Kc167 cells and disrupts contractile ring assembly in Drosophila S2 cells at a concentration of 40 μM, highlighting the critical role of Aurora B kinase in cell division.
