Aurora Kinase Inhibitor

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

SCH-1473759 is an aurora inhibitor with IC₅₀s of 4 and 13 nM for aurora A and B, respectively.

SCH-1473759 hydrochloride is an aurora inhibitor with IC₅₀s of 4 and 13 nM for aurora A and B, respectively.

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 H3^Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with K_d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K_d values ranging from 55-456 nM.

GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.1. GSK2646264 also inhibits other kinases with pIC₅₀ values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.

PLK4-IN-1 is a spiro cyclopropyl indolinone compound and PLK4 inhibitor with inhibitory activity against Aurora A and Aurora B kinases .PLK4-IN-1 can be used for the research of cancer .

TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (K_i=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (K_i=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity.

DBPR728 is an acyl prodrug of 6K465 that carries fewer hydrogen bond donors. 6K465 acts as an Aurora kinase inhibitor that destabilizes MYC family cancer proteins and has antitumor efficacy. DBPR728 has the potential to inhibit cancers that overexpress C-MYC and N-MYC, with a 10-fold increase in oral bioavailability compared to 6K465.

EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of ^L858R EGFR and AURKB with IC₅₀s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research.

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. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI₅₀ values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis.

6K465 is a pyrimidine-based Aurora A (AURKA) inhibitor. 6K465 can reduce the levels of c-MYC and N-MYC oncoproteins, demonstrating anticancer activity.

Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC₅₀s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.

AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC₅₀ of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.

Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (K_d) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma.

Ceftriaxone (Standard) is the analytical standard of Ceftriaxone. This product is intended for research and analytical applications. Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis[1][2][3][4][5][6][7].

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

Aurora kinase-IN-8 is a orally active Aurora kinase inhibitor. Aurora kinase-IN-8 shows IC₅₀ values of 2.8 and 28.1 nM against Aurora A kinase and Aurora B kinase. Aurora kinase-IN-8 can prevent spindle formation, cause G2/M phase arrest, and induce cell apoptosis. Aurora kinase-IN-8 can be used for the research of cancer, such as triple-negative breast cancer.

Aurora kinase inhibitor-8 is a highly selective inhibitor of the Aurora kinases.

Protein kinase inhibitor 6 is a protein kinase inhibitor.

Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC₅₀ of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells.