Aurora Kinase

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  1. Aurora A inhibitor.

    6K465 is a pyrimidine-based small molecule inhibitor selectively targeting Aurora A kinase (AURKA). By inhibiting AURKA activity, 6K465 effectively reduces the expression levels of the oncogenic transcription factors c-MYC and N-MYC, contributing to its anticancer effects. This compound shows promise as a therapeutic agent for MYC-driven cancers by disrupting mitotic regulation and oncogene stabilization.
  2. Aurora kinase inhibitor

    Derrone is a prenylated isoflavone that functions as an Aurora kinase inhibitor, exhibiting IC₅₀ values of 6 μM for Aurora B and 22.3 μM for Aurora A. By targeting these key mitotic kinases, Derrone disrupts cell cycle progression and displays notable antitumor activity, making it a promising compound for cancer research focused on mitotic regulation.
  3. Aurora-A Inhibitor

    PHA-680626 is a selective inhibitor of Aurora-A kinase, disrupting its interaction with N-Myc. This compound effectively inhibits the kinase activities of both AURKA and Bcr-Abl, leading to the degradation of N-Myc. Additionally, PHA-680626 reduces phosphorylation levels of CrkL and histone H3. Its anti-proliferative and pro-apoptotic effects have been demonstrated in Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ hematopoietic stem cells, making it a valuable tool for research in cancer therapeutics.
  4. Aurora kinase Inhibitor

    Aurora kinase-IN-8 is an orally active inhibitor of Aurora kinases, specifically targeting Aurora A and B kinases with IC50 values of 2.8 nM and 28.1 nM, respectively. This compound effectively disrupts spindle formation, induces G2/M phase arrest, and promotes apoptosis in cancer cells. It is particularly relevant for research applications focused on malignancies, including triple-negative breast cancer.
  5. Aurora A Kinase Inhibitor

    Alisertib sodium is a selective inhibitor of Aurora A kinase, exhibiting an IC50 of 1.2 nM. This compound disrupts mitotic spindle formation and leads to mitotic accumulation, thereby inducing apoptosis and autophagy in leukemic cells via the AKT/mTOR/AMPK/p38 signaling pathway. Alisertib sodium demonstrates significant antitumor activity, making it a valuable reagent for cancer research and therapeutic applications.
  6. Aurora B Inhibitor

    Barasertib dihydrochloride is a selective inhibitor of Aurora B kinase, exhibiting an IC50 of 0.37 nM in cell-free assays. This compound effectively induces growth arrest and apoptosis in various cancer cell lines, making it a valuable tool for cancer research. Its mechanism of action provides insights into the role of Aurora B in cell cycle regulation and tumorigenesis.
  7. Aurora/JAK Inhibitor

    AT9283 lactic acid is a multi-targeted kinase inhibitor primarily targeting Aurora A/B and JAK2/3. It demonstrates potent biological activity against various cancers, exhibiting IC50 values between 1 to 30 nM for its targets. AT9283 lactic acid effectively inhibits the growth and survival of multiple solid tumors in both in vitro and in vivo models, making it a valuable reagent for cancer research applications.
  8. Aurora A/Aurora B/HDAC1/HDAC2 Inhibitor

    Aurora kinase/HDAC-IN-1 is a potent dual inhibitor targeting Aurora A, Aurora B, HDAC1, and HDAC2. This compound promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis through G2/M cell-cycle arrest. It demonstrates significant antiproliferative activity in colorectal cancer cells, with an IC50 of 30.2 nM in HCT-116 cells, and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models. This reagent is valuable for research in cancer biology and therapeutic application development.
  9. Aurora Kinase A/JAK2 Inhibitor

    AJI-100 is a dual-target inhibitor that selectively inhibits Aurora kinase A and JAK2 with IC50 values of 12.7 nM and 18.5 nM, respectively. By directly blocking Aurora kinase A, AJI-100 disrupts T cell mitosis and cell polarity, while its inhibitory effect on JAK2 activation prevents STAT3 phosphorylation. This compound is valuable for research focused on modulating immune responses and has potential applications in the prevention of graft-versus-host disease (GVHD).
  10. Aurora-A kinase Inhibitor

    LY3295668 erbumine is a potent and selective inhibitor of Aurora-A kinase, exhibiting a Ki value of 0.8 nM for AurA while demonstrating significantly lower binding affinity for AurB at 1038 nM. This compound effectively inhibits the autophosphorylation of Aurora-A, leading to mitotic arrest and apoptosis without promoting polyploidy associated with AurB inhibition. LY3295668 erbumine is valuable for research into small cell lung cancer and other conditions involving dysregulation of Aurora kinases.
  11. Aurora B Inhibitor

    HOI-07 is a selective inhibitor of Aurora B kinase that interferes with the phosphorylation of histone H3 at Ser10 in lung cancer cells. This compound induces cell-cycle arrest and apoptosis, demonstrating significant antitumor activity. HOI-07 effectively suppresses tumor growth in xenograft models, including A549, 143B, and KHOS, making it a valuable tool for cancer research and therapeutic investigation.
  12. Aurora Kinase Inhibitor

    Aurora Kinase Inhibitor-14 is a highly selective inhibitor of Aurora kinases, demonstrating IC50 values of 0.5 nM for Aurora A and 1.2 nM for Aurora B. This compound binds to the ATP-binding site of these kinases, effectively disrupting chromosome segregation during mitosis and promoting apoptosis in tumor cells. Aurora Kinase Inhibitor-14 is a valuable tool for investigating the therapeutic potential in various solid tumors and hematological malignancies, including non-small cell lung cancer, breast cancer, and acute myeloid leukemia.
  13. Aurora A Inhibitor

    Aurora A Inhibitor 2 is a potent inhibitor of Aurora A kinase, exhibiting an IC50 value of 21.94 nM. This compound has been shown to induce caspase-dependent apoptosis in MDA-MB-231 cells, highlighting its potential as a therapeutic agent in cancer research. It is useful for studies investigating the role of Aurora A in cell cycle regulation and apoptosis.
  14. Aurora/VEGF/PDGF Inhibitor

    Ilorasertib hydrochloride is a potent, orally active inhibitor targeting Aurora kinases, with IC50 values of 116 nM, 5 nM, and 1 nM for Aurora A, B, and C, respectively. Additionally, it exhibits significant inhibition of VEGF and PDGF pathways. This compound is valuable for research related to acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS), facilitating studies into the mechanisms of these hematologic malignancies.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. Aurora Kinase Inhibitor

    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.
  49. Aurora A Inhibitor

    Aurora A inhibitor 4 (compound C9) is a selective inhibitor of Aurora A kinase, demonstrating a GI50 of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells. This compound exhibits significant anti-proliferative effects, making it valuable for research focused on cell cycle regulation and cancer therapeutics. Its ability to inhibit Aurora A activity can be applied in studies investigating mitotic dysregulation in various tumor types.
  50. Aurora Kinase Inhibitor

    Aurora B inhibitor 1 is a selective inhibitor of the Aurora B kinase, exhibiting a Ki value of <0.010 µM. This compound plays a crucial role in manipulating cell division and is instrumental in research surrounding cancer biology and therapeutic development. Its ability to inhibit Aurora B activity makes it a valuable tool for studies focused on mitotic regulation and chromosomal instability.

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