Aurora Kinase

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  1. human A3 adenosine receptor antagonist /Aurora inhibitor

    Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
  2. Aurora Kinase inhibitor

    VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.
  3. MEK/Aurora Inhibitor

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
  4. Aurora Kinase B inhibitor

    AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases.
  5. Aurora A Kinase inhibitor

    MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..
  6. Aurora/JAK inhibitor

    AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.
  7. Aurora Kinase inhibitor

    AMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
  8. Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor

    R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.
  9. Aurora inhibitor

    Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
  10. Aurora A Kinase inhibitor

    MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.
  11. Aurora B Kinase inhibitor

    Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
  12. CDK/Aurora A/B Inhibitor

    JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
  13. IGF-1R, Aurora, FGFR, ABL, SRC inhibitor

    XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
  14. Aurora Kinase B/C inhibitor

    GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.

  15. Aurora A/B Kinase inhibitor

    PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
  16. multi-kinase inhibitor

    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3.
  17. Aurora B inhibitor

    HOI-07 is a potently Aurora B kinase inhibitor.
  18. Aurora A Inhibitor

    LY3295668, also known as AK-01, is potent Aurora-A kinase inhibitor.
  19. Aurora inhibitor

    Aurora inhibitor 1 is a potent Aurora inhibitor with an IC50 of ?? 4 nM and ??13 nM for Aurora A and Aurora B kinase, respectively.
  20. Aurora/PLK dual inhibitor

    AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis.
  21. Aurora A kinase inhibitor

    Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM.
  22. Aurora B inhibitor

    AZD1152 is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML).
  23. Aurora Kinase A Inhibitor

    MK-8745 is a novel Aurora-A specific inhibitor. It induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages.
  24. Aurora kinase A inhibitor

    TC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity.
  25. Aurora A/B inhibitor

    SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
  26. Aurora Kinase inhibitor

    SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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