Aurora B 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).

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.

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.

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.

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.

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.