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Aurora kinase inhibitors block Aurora A, Aurora B and Aurora C, three serine/threonine kinases that coordinate mitosis. The founding aurora gene was described in Drosophila in 1995, where its mutations prevented centrosome separation and produced monopolar spindles. In human cells Aurora A acts at centrosomes and spindle poles during spindle assembly. Aurora B belongs to the chromosomal passenger complex, which moves from centromeres to the spindle midzone during division. Alisertib preferentially inhibits Aurora A, whereas barasertib-HQPA and hesperadin mainly target Aurora B. Work with hesperadin in 2003 linked Aurora B to correcting kinetochore-microtubule attachments and maintaining the spindle assembly checkpoint. Tozasertib and AMG 900 inhibit all three family members and are used as pan-Aurora tools.
dAURK-4 hydrochloride is a potent and selective PROTAC degrader targeting Aurora A kinase (AURKA), derived from the AURKA inhibitor Alisertib. It effectively induces AURKA degradation and exhibits notable anticancer activity, making it a valuable agent for studying AURKA-driven oncogenic pathways and therapeutic development.
JB170 is a potent PROTAC-mediated degrader targeting AURORA-A kinase, with a DC50 of 28 nM. By conjugating Alisertib with the Cereblon-binding molecule Thalidomide, JB170 selectively binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). The compound induces S-phase cell cycle arrest specifically via the depletion of AURORA-A and effectively inhibits its non-catalytic functions. JB170 serves as a valuable tool for studying AURORA-A's roles in cellular processes and therapeutic applications in cancer research.
dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM). It effectively induces the degradation of these kinases, leading to reduced N-Myc levels and decreased viability in IMR32 neuroblastoma cells. dAurAB5 also downregulates AAK1, PTK2, GAK, and TTK, making it a valuable tool for investigating the molecular mechanisms in neuroblastoma and related cancers.
HLB-0532259 is a PROTAC degrader targeting Aurora-A and N-Myc, designed to selectively induce the degradation of these oncoproteins. In non-MYCN amplified MCF-7 cells, HLB-0532259 shows a degradation concentration (DC50) of 20.2 nM for Aurora-A, while in MYCN amplified SK-N-BE and Kelly cells, it demonstrates DC50 values of 179 nM and 229 nM for N-Myc, respectively. This compound has also exhibited significant antitumor efficacy in mouse models, making it a valuable reagent for cancer research focusing on targeted protein degradation.
dAurAB2 is a dual-targeting PROTAC designed to degrade Aurora-A and Aurora-B, demonstrating potent efficacy with DC50 values of 59 nM and 39 nM, respectively. This compound effectively reduces N-Myc protein levels in MYCN-amplified IMR32 neuroblastoma cells, making it a valuable tool for neuroblastoma research. The unique design incorporates a specific Aurora ligand and an E3 ligase ligand connected by a tailored linker, facilitating targeted degradation and advancing studies in cancer biology.
AurAP14 is a PROTAC degrader specifically targeting Aurora A, with a DC50 of 120 nM. This compound exhibits potent inhibitory effects on various tumor cell lines, showing IC50 values of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis while effectively arresting A549 cells in the S and G2/M phases of the cell cycle. Additionally, AurAP14 demonstrates significant anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR, making it a valuable tool for research focused on treating Aurora A-overexpressing non-small cell lung cancer (NSCLC).
PROTAC Aurora A Degrader-1 is a selective degrader that targets Aurora A, effectively forming a ternary complex with AURKA and CRBN. This compound demonstrates potent biological activity, inducing degradation of AURKA, lowering MYCN levels, and promoting DNA damage and apoptosis in cancer cells. With DC50 values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively, it exhibits significant antiproliferative effects and is valuable for research on neuroblastoma and small cell lung cancer.
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