aurora

Hesperadin(IC50=250 nM) effectively inhibits Aurora B. It potently reduces the activity of AMPK, MAPKAP-K1, MKK1, Lck, CHK1 and PHK, but it could not inhibit MKK1 activity in vivo.

Aurora inhibitor 1 is a potent inhibitor of Aurora A and Aurora B kinases with IC50 values of ≤ 4 nM and ≤ 13 nM, respectively.

Aurora B inhibitor 1 is an Aurora B (Aurora-1) inhibitor (Ki <0.010 µM) with potential anticancer activity for cancer research.

Aurora-A ligand 1 is a potent and selective inhibitor of Aurora-A, exhibiting a dissociation constant (Kd) of 0.85 nM. It serves as a target protein ligand [PROTAC target protein ligand] in the development of PROTAC Aurora-A degraders with antitumor activity. Additionally, Aurora-A ligand 1 is utilized in the synthesis of HLB-0532259, which exhibits antitumor effects against neuroblastoma.

Aurora A inhibitor4 (compound C9) is a potent inhibitor of Aurora A, with GI50 values of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells.

Aurora kinase inhibitor-13 (Compound 2) is an inhibitor of Aurora kinase, with an IC50 value of 2.3 μM for Aurora kinase A.

BET/Aurora kinase-IN-1 (Compound 38) is a dual inhibitor of BET and Aurora kinases. It exhibits antiproliferative activity against various tumor cell lines and demonstrates significant antitumor efficacy in xenograft models of renal cell carcinoma and colon cancer, with tumor growth inhibition (TGI) rates of 45.99% and 53.06%, respectively.

Aurora kinase-IN-7 (compound 4b) is an orally active inhibitor selectively targeting AURKB. It is utilized in the study of aggressive cancers.

Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases, effectively inhibiting both Aurora A and Aurora B with IC50 values of 0.5 nM and 1.2 nM, respectively. It binds to the ATP binding site of Aurora kinases, blocking chromosome separation during mitosis and inducing apoptosis in tumor cells. Aurora kinase inhibitor-14 shows potential for research in various solid tumors and hematologic malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia.

MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases, with IC50 values of 0.56 μM and 0.16 μM, respectively. This compound exhibits broad-spectrum anticancer activity, demonstrating potent effects against NCI-60 cancer cell lines, including SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM. By inhibiting Aurora A and MASTL kinases, MASTL/Aurora A-IN-1 induces G2/M phase cell cycle arrest, thereby impeding cancer cell proliferation. This compound is applicable for cancer research, particularly in the study of tumors with mitotic dysregulation.

Aurora kinase inhibitor-12 (Compound 1a) is an inhibitor targeting aurora kinase, a crucial enzyme involved in tumor growth.

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

Aurora/LIM kinase-IN-1 (Compound F114) is a potent dual inhibitor of aurora and LIM kinases. It inhibits the proliferation and invasion of glioblastoma multiforme (GBM), making it a potential candidate for drug development in GBM and other cancers. Aurora and LIM kinases are involved in neoplastic cell division and cell motility, respectively [1].

Aurora Kinases-IN-2 (compound 12Aj) is a potent inhibitor of Aurora kinases, with IC50 values of 90 nM for Aurora A and 152 nM for Aurora B, and is applicable in cancer research.

Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM.

Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B bipolar kinase inhibitor with an IC50 of 0.093 μM for Aurora A and 0.09 μM for Aurora B, demonstrating broad-spectrum anti-proliferative activity.

Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, θ), exhibiting inhibitory activity on AurA (IC50: 6.9 nM) and PKCα (IC50: 16.9 nM), and demonstrating anti-proliferative and anti-metastatic effects on breast cancer cells.

Aurora A inhibitor 1 is a potent and selective inhibitor of Aurora A, a protein associated with cancers of multiple histological origins that may exhibit oncogenic activity when overexpressed. Aurora A inhibitor 1 exhibits potential for studies related to Aurora A-mediated cancer diseases.

Aurora kinase inhibitor-8 (highly selective) inhibits Aurora kinase.

Aurora kinase inhibitor-10 is an orally active Aurora B inhibitor (IC50: 8 nM) that exhibits antitumour effects.

Aurora Kinases-IN-3, an orally active inhibitor of AURKB, suppresses AURKB activity by hindering its mitotic localization rather than by inhibiting its phosphorylation of H3 at Ser10.

Aurora kinase-IN-1, a potent aurora kinase inhibitor, modulates cell cycle progression and induces apoptosis by upregulating G1 cell cycle inhibitory proteins (including p21 and p27), elevating G1 progressive cyclin D1, and downregulating G1-to-S progressive cyclins, thereby arresting the cell cycle at the G1/S boundary. It stands as a promising lead compound for the development of chemotherapeutic agents.

Aurora Kinases-IN-4 (Compound 11c) is a covalent, ATP-competitive inhibitor of aurora kinase A with an IC50 value of 1.7 nM. It inhibits cell proliferation in SJSA-1, MDA-MB-231, A549, and HeLa cell lines with IC50 values of 4.27, 1.54, 3.08, and 6.99 μM, respectively. This compound is applicable in research concerning triple-negative breast cancer (TNBC) [1].

Aurora A Inhibitor 3 (Compound 5h) effectively inhibits Aurora-A kinase, exhibiting an IC50 of 0.78 μM, and demonstrates cytotoxicity against MCF-7 and MDA-MB-231 cell lines with GI50 values of 0.12 μM and 0.63 μM, respectively [1].