aurora-a

Aurora-A ligand 1 is a potent and selective inhibitor of Aurora-A, exhibiting a dissociation constant (Kd) of 0.85 nM. It serves as a target protein ligand [PROTAC target protein ligand] in the development of PROTAC Aurora-A degraders with antitumor activity. Additionally, Aurora-A ligand 1 is utilized in the synthesis of HLB-0532259, which exhibits antitumor effects against neuroblastoma.

dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50= 8.8 nM) and Aurora-B (DC50= 6.1 nM). It induces the degradation of Aurora-A and Aurora-B, leading to reduced N-Myc levels and decreased viability of IMR32 neuroblastoma cells. Additionally, dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. This compound is applicable in cancer research, including neuroblastoma.

JB170 is a highly efficient and specific Aurora A degradator (DC50 = 28 nM). The PROTAC is composed of Alisertib and Thalidomide, with an EC50 value for AURORA-A that is ten times that of AURORA-B. It induces S-phase arrest in cell growth and inhibits the non-catalytic function of the AURORA-A kinase.

PROTAC MPS1 degrader 1 (Compound 19) acts as a potent degrader of Monopolar spindle 1 (Mps1, TTK), AURKA, and AURKB, with DC50 values of 17.7, 108.7, and 570.3 nM respectively. It is utilized in the study of acute myeloid leukemia. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase)

JB300 is a PROTAC-based compound that serves as a highly selective degrader of Aurora A, with a DC50 of 30 nM. It is utilized in cancer research. JB300 comprises the PROTAC target protein ligand MK-5108 [pink part], E3 ligase ligand Thalidomide-O-COOH [blue part], and PROTAC Linker Boc-NH-PEG2-C2-NH2 [black part]. The conjugate of the E3 ubiquitin ligase ligand and linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc.

HLB-0532259 is a PROTAC degrader that targets the degradation of Aurora-A and N-Myc. In non-MYCN amplified MCF-7 cells, it degrades Aurora-A with a DC50 of 20.2 nM, and in MYCN amplified SK-N-BE and Kelly cells, it degrades N-Myc with DC50 values of 179 nM and 229 nM, respectively. HLB-0532259 has demonstrated antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligaseCereblon)

dAurAB2 is a bifunctional PROTAC capable of effectively degrading Aurora-A and Aurora-B, with DC50 values of 59 nM and 39 nM, respectively. It reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells and is valuable for neuroblastoma research.

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.

MS44 is a potent degrader of aurora kinase B (AURKBPROTAC) with a degradation concentration (DC50) of 103 nM. It effectively and selectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner, showing specificity for AURKB over AURKA and AURKC. MS44 inhibits the proliferation of various cancer cell lines and strongly induces G2/M arrest. It is useful for studying AURKB-dependent tumors.

TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.