Aurora Kinase Degrader

CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The K_D values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC₅₀ against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.

dAurAB5 is a dual Aurora-A (DC₅₀ = 8.8 nM) and Aurora-B (DC₅₀ = 6.1 nM) PROTAC degrader. dAurAB5 induces degradation of Aurora-A and Aurora-B, reduces N-Myc levels, and decreases viability in IMR32 neuroblastoma cells. dAurAB5 downregulates the levels of AAK1, PTK2, GAK, and TTK. dAurAB5 can be used to study cancers such as neuroblastoma. (Pink: TTK ligand 2: HY-168542, Blue: Thalidomide-O-COOH: HY-103597, Black: 6-Aminocaproic acid: HY-B0236).

SK2188 (JB325) is a highly efficient and selective PROTAC degrader targeting AURKA (DC₅₀ = 3.9 nM). SK2188 induces DNA damage and cell apoptosis. SK2188 indirectly degrades MYCN, inhibits tumor cell proliferation, and provides insights into the study of MYCN-amplified neuroblastoma.

SK2187 (JB301) is a selective AURKA PROTAC degrader with a DC₅₀ of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC₅₀ of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma.

HLB-0532259 is a Aurora-A/N-Myc PROTAC degrader, with a DC₅₀ of 20.2 nM against Aurora-A in MCF-7 cells; its DC₅₀ values against N-Myc are 179 nM in SK-N-BE (2) cells and 229 nM in Kelly cells, respectively. HLB-0532259 induces apoptosis (apoptosis) in MYCN-amplified neuroblastoma cells and inhibits tumor growth in mouse xenograft models. HLB-0532259 can be used for the research of neuroblastoma.

PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC₅₀ values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia.

dAURK-4 hydrochloride is a selective AURKA PROTAC degrader. dAURK-4 hydrochloride promotes ubiquitination and degradation of AURKA. dAURK-4 hydrochloride can be used in the research of glioblastoma and multiple myeloma.

MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC₅₀ = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand.

AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC₅₀s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker).

PROTAC AURKA degrader 2 (compound D) is a potent and selective PROTAC AURKA degrader with an IC₅₀ of 3.58 nM. PROTAC AURKA degrader 2 exhibits 21.6-fold selectivity for AURKA over AURKB (IC₅₀ = 77.2 nM). PROTAC AURKA degrader 2 specifically depletes AURKA on the mitotic spindle.

dAurAB2 is a dual-degrading PROTAC that potently degrades Aurora-A and Aurora-B with DC₅₀s of 59 nM and 39 nM, respectively. dAurAB2 reduces N-Myc levels in MYCN-amplified IMR32 neuroblastoma cells. dAurAB2 can be used for the study of neuroblastoma. (Pink, Aurora ligand (HY-10804); Blue, E3 ligand: (HY-103597); Black, linker (HY-W105740)).

JB300 is a highly selective Aurora A degrader based on PROTAC technology (DC₅₀=30 nM). JB300 can be used for tumor research. JB300 consists of PROTAC target protein ligand MK-5108 (HY-13252) (pink part), E3 ligase ligand Thalidomide-O-COOH (HY-103597) (blue part) and PROTAC Linker Boc-NH-PEG2-C2-NH2 (HY-W008474) (black part), of which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc (HY-172145).

SK5527 is a selective AURKA PROTAC degrader degrading AURKA with DC₅₀ = 2 nM. SK5527 bind to NanoLuc-AURKA with an IC₅₀ of 20 nM. SK5527 effectively reduces MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK5527 efficiently reduced AURKA levels in vivo. SK5527 can be used for neuroblasto2ma research.

dAURK-4 is a selective AURKA PROTAC degrader. dAURK-4 promotes ubiquitination and degradation of AURKA. dAURK-4 can be used in the research of glioblastoma and multiple myeloma.

PROTAC AURKA degrader 1 (Compound A16 + X7) is a Aurora kinase A (AURKA) PROTAC degrader. PROTAC AURKA degrader 1 can be used for cancers research. Pink: AURKA ligand (HY-175827); Blue: CRBN ligase ligand (HY-W867704); Black: linker (HY-132208)

SK4454 is a selective AURKA PROTAC degrader degrading AURKA with IC₅₀ = 8 nM. MYCN levels in MYCN-amplified neuroblastoma cells and limited by MDR1-mediated efflux. SK4454 efficiently reduced AURKA levels in vivo. SK4454 can be used for neuroblastoma research.

Abd141 is a dual PROTAC degrader of ATR and Aurora kinase A (AURKA), with DC₅₀ values of 97.7 nM and 6.7 nM, respectively. Abd141 inhibits the proliferation of acute lymphoblastic leukemia cells. Abd141 can be used in the research of acute lymphoblastic leukemia.

M9101 is a selective Aurora A PROTAC degrader with a DC₅₀ of 2.3 nM. M9101 induces G2/M arrest in triple-negative breast cancer cells and potently inhibits the proliferation of multiple tumor cell lines. M9101 can be used in the research of various cancers including triple-negative breast cancer.

PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC₅₀ value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G₂/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer.

PROTAC Aurora A Degrader-1 (Compound 280) is a blood-brain barrier-permeable selective Aurora A PROTAC degrader, with DC₅₀ values of 1 nM and 2 nM in LAN5 and SMS-SAN cells, respectively. PROTAC Aurora A Degrader-1 induces the formation of a ternary complex between AURKA and CRBN, degrades AURKA, reduces MYCN levels, induces DNA damage and apoptosis, exerts antiproliferative activity in cancer cells, and regulates the immune system. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer.