Aurora Kinase Inhibitor

KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC₅₀ = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer.

Aurkin A is an allosteric inhibitor for the interaction between Aurora A Kinase (also known also Aurka) and TPX2, through targeting the TPX2 binding sites with K_d of 3.77 μM. Aurkin A can disrupt polyploidy induced by Alisertib (HY-10971) and increase apoptosis of tumor cells. Aurkin A can be used in research on mitosis and cancer.

Gossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.

Aurora kinase-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10.

MKI-3 is a selective microtubule-associated serine/threonine kinase-like (MASTL) inhibitor with an IC₅₀ of 5.72 nM and a K_d of 1.89 nM. MKI-3 disrupts the MASTL-ENSA-Aurora A signaling axis. MKI-3 induces chromosomal instability, mitotic catastrophe and apoptosis (apoptosis) in cancer cells. MKI-3 is applicable to research related to triple-negative breast cancer.

CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC₅₀ of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer.

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.

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.

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

Protein kinase inhibitor 6 is a protein kinase inhibitor.

Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

Barasertib (AZD1152 dihydrochloride), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay. Barasertib (AZD1152 dihydrochloride) induces growth arrest and apoptosis in cancer cells.

Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC₅₀: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC₅₀s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC).

KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC₅₀ = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer.

ATC12 is a Aurora-A kinase inhibitor. ATC12 binds to Aurora-A and competes with TPX2 for binding to disrupt the Aurora-A/TPX2 interaction. ATC12 inhibits cancer cell proliferation, induces apoptosis and cellular senescence. ATC12 can be used in the research of breast cancer.