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.

Aurora-A ligand 2 serves as a target protein ligand for PROTAC. It is utilized in the synthesis of [SK4454].

dAURK-4 hydrochloride is a selective AURKA (Aurora A) degrader with anticancer and antiproliferative activities. dAURK-4 hydrochloride has been shown to be an anticancer and antiproliferative agent.

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.

AurAP14 is an Aurora APROTAC degrader with a DC50 of 120 nM. It exhibits notable inhibitory activity against various tumor cell lines, with an IC50 of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis in A549 cells and causes cell cycle arrest in the S and G2/M phases. It demonstrates antitumor efficacy in both A549 and A549/PTR nude mouse xenograft models. AurAP14 is applicable for studying treatments for non-small cell lung cancer (NSCLC) with Aurora A overexpression.

PROTACAURKA degrader 2 (compound D) is a potent and selective degrader for PROTACAURKA, with an IC50 of 3.58 nM. It demonstrates 21.6 times greater selectivity for AURKA compared to AURKB (IC50 = 77.2 nM) and specifically depletes AURKA on the mitotic spindle.

SK4454 is a selective AURKAPROTAC degrader that targets the AURKA protein with an IC50 of 8 nM. It binds to NanoLuc-AURKA with an IC50 of 20 nM. SK4454 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells, although its activity is limited by MDR1-mediated efflux. In vivo, SK4454 efficiently decreases AURKA levels. It is useful for research related to neuroblastoma.

SK5527 is a selective AURKA PROTAC degrader that targets and degrades the AURKA protein, exhibiting a DC50 of 2 nM. It binds to NanoLuc-AURKA with an IC50 of 20 nM. In MYCN-amplified neuroblastoma cells, SK5527 effectively reduces MYCN levels, but its activity is constrained by MDR1-mediated efflux. In vivo, it efficiently lowers AURKA levels. SK5527 serves as a useful tool for neuroblastoma research.

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.

AURKA-IN-4 is a novel capsaicin analog that acts as an Aurora kinase A (AURKA) inhibitor. By specifically targeting AURKA in mitochondria, AURKA-IN-4 inhibits AURKA-dependent mitophagy, thereby eliminating the organelle. AURKA-IN-4 exhibits antiproliferative effects against various tumor cells and holds potential value for application in anticancer therapies that target cell cycle regulation.

PROTACAURKA degrader 1 (Compound A16 + X7) is a PROTAC degrader targeting Aurora kinase A (AURKA), useful in cancer research.

MK-5108-NH-PEG2-alkyne is an Aurora kinase A (AURKA) inhibitor. It is utilized in the synthesis of PROTAC AURKA degrader 1.

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.

dAURK-4, a derivative of Alisertib, functions as a potent and selective degrader of AURKA (Aurora A), exhibiting anticancer properties [1].