aurora kinase a

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-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.

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

Aurora kinaseligand-1 (Compound I-4) is an AURKB PROTAC ligand designed to target aurora kinase B. It can conjugate with an E3 ligase ligand and a linker to form the AURKB PROTAC degrader MS44, which is applicable in cancer research.

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

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 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).

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

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.

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

Cenisertib is A potent ATP-competitive multi-kinase inhibitor, showing inhibitory effects on the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5, FLT3, as well as kinase inhibitors of FER and its homolog. Cenisertib inhibits the growth of tumor mast cells (MCS) by inhibiting the activity of several different molecular targets. Cenisertib also inhibits tumor growth in pancreatic, breast, colon, ovarian and lung cancer and leukemia in xenograft models.

LY3295668 (AK-01) is a selective inhibitor of Aurora A, with Ki values of 0.8 nM for Aurora A and 1038 nM for Aurora B.

XU1(Benzo[c][1,8]naphthyridin-6(5h)-One) is an Aurora protein kinase inhibitor used for the treatment of diseases suitable for inhibition, regulation or modulation of kinase signaling.

H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

KW-2450 Formate is an IGF-1R/IR tyrosine kinase inhibitor with antitumor effects that acts through inhibition of Aurora A and B kinases.KW-2450 Formate inhibits the growth of TNBC xenografts and induces tetraploid accumulation.

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM.

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