aurora

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 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].

Aurora Kinase Inhibitor-11 (compound 25) acts as an inhibitor against Aurora Kinase, exhibiting a potent IC50 of 0.14 μM. The compound also demonstrates anticancer activity [1].

FAK aurora kinase-IN-1, a dual inhibitor of FAK and aurora kinase, has IC50 values of 6.61 nM and 0.91 nM respectively, and demonstrates anticancer effects (WO2018019252A1; compound 11) [1].

Aurora kinase inhibitor-2 (IUN-70219) is a cell-permeable anilinoquinazoline that inhibit the activity of Aurora A (IC50 = 0.39 M).

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

SP600125 (JNK Inhibitor II) is a JNK inhibitor that inhibits JNK1, JNK2, and JNK3 (IC50=40 40 90 nM) with oral potency, reversibility, and ATP-competitive properties. SP600125 inhibits autophagy and induces apoptosis.