Aurora Kinase Inhibitor

Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC₅₀ value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI₅₀ values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively.

(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo.

PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells.

CDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC₅₀ value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC₅₀ = 26.3 nM), moderate inhibitory effects on Aurora A (IC₅₀ = 92.0 nM) and CDK9 (IC₅₀ = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC₅₀ > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer.

BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively.

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC₅₀ values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.

SNS-314 is a potent and selective aurora kinase inhibitor with IC₅₀s of 9, 31, and 6 nM for aurora A, B and C, respectively.

MLN8054 sodium is an Aurora A inhibitor with radiosensitivity-enhancing activity. MLN8054 sodium can activate the DNA double-strand break reaction of prostate cancer cells in in vitro experiments. The application of MLN8054 sodium is closely related to accumulation in the G2/M phase of the cell cycle and polyploid formation. In vivo experiments show that MLN8054 sodium can significantly delay the growth of prostate cancer tumors and promote tumor cell apoptosis when used in combination with radiotherapy.

Aurora kinase-IN-7 (compound 4b) is an orally active and selective AURKB inhibitor. Aurora kinase-IN-7 can be used in the study of aggressive cancers.

Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC₅₀ of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity.

Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC₅₀s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity.

Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC₅₀ of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity.

Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC₅₀ values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.

Aurora kinase-IN-15 is a potent dual Aurora A and Aurora B kinase inhibitor. Aurora kinase-IN-15 has broad-spectrum anticancer activity and low toxicity to normal cells. Aurora kinase-IN-15 induces G₂/M phase arrest, apoptosis, and activates the intrinsic apoptotic pathway through upregulation of Caspase 3 and Bax, along with downregulation of Bcl-2. Aurora kinase-IN-15 can be used for the study of breast cancer, hepatocellular carcinoma, colorectal cancer and prostate cancer.

Aurkb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Aurkb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

XMD-12 (compound 1) is an Aurora kinase (Aurora Kinase) inhibitor with anti-tumor activity that promotes paclitaxel (HY-B0015) induced cell death. XMD-12 exhibits high selectivity and potency against Aurora A, B, and C kinases, with IC₅₀ values of 5.6, 18.4, and 24.6 nM, respectively.

Palmatine (chloride) (Standard) is the analytical standard of Palmatine (chloride). This product is intended for research and analytical applications. Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

Aurora/LIM kinase-IN-1 (Compound F114) is a potent and dual inhibitor of aurora and lim kinase. Aurora kinases and lim kinases are involved in neoplastic cell division and cell motility, respectively. Aurora/LIM kinase-IN-1 inhibits GBM proliferation and invasion. Aurora/LIM kinase-IN-1 is a promising new scaffold for dual aurora/lim kinase inhibitors that may be used in future agent development efforts for GBM, and potentially other cancers.

AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC₅₀: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA.

Aurkc Mouse Pre-designed siRNA Set A contains three designed siRNAs for Aurkc gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.