Aurora A Degrader

TL12-186 is a multi-kinase PROTAC degrader. TL12-186 recruits the CRBN E3 ubiquitin ligase to target and degrade a variety of distinct kinases, including FLT3, BTK, AURKA, PTK2B, and multiple cyclin-dependent kinases (CDKs). TL12-186 can be used in leukemia-related research.

dAurAB5 is a potent Aurora-A/Aurora-B PROTAC degrader with DC₅₀ values of 8.8 nM and 6.1 nM, respectively. dAurAB5 promotes proteasomal degradation of target proteins, induces ubiquitination of Aurora-A and Aurora-B kinases, and downregulates the protein levels of TTK and MYCN. dAurAB5 can be used in studies related to neuroblastoma[1].

SK2188 (JB325) is a selective AURKA PROTAC degrader with a DC₅₀ of 3.9 nM. SK2188 recruits CRBN E3 ubiquitin ligase to target and degrade AURKA, abrogating both its catalytic and non-kinase functions, which leads to the destabilization and degradation of the oncogenic protein MYCN, ultimately inducing replication stress, DNA damage and apoptosis. SK2188 is applicable to research related to neuroblastoma.

SK2187 (JB301) is a selective AURKA PROTAC degrader. SK2187 induces targeted degradation of AURKA by recruiting the CRBN E3 ubiquitin ligase. SK2187 is applicable to research related to 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.

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.

AurAP14 is an Aurora A PROTAC degrader (DC₅₀ = 120 nM). AurAP14 can form a stable ternary complex with Aurora A kinase and HSP90, recruiting cullin family E3 ubiquitin ligases and MDM2 to mediate the ubiquitination and proteasome degradation of Aurora A kinase. AurAP14 increases p53 levels and decreases C-MYC levels; AurAP14 induces Apoptosis. AurAP14 can be used in the study of non-small cell lung cancer.

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.

JB300 is a PROTAC degrader that selectively targets and degrades AURORA-A by recruiting cereblon, with EC₅₀ values of 373 nM and 193 nM in intact cells and permeabilized cells, respectively. JB300 can be used in studies related to acute myeloid leukemia and targeted protein degradation mechanisms.

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.

AURKA-IN-4 is a Capsaicin (HY-10448)-derived molecular glue targeting AURKA-PHB2, and acts as an inhibitor of Aurora kinase A (AURKA) and PHB2. AURKA-IN-4 binds to the active site of AURKA and the inhibitory pocket of PHB2, inhibits AURKA-dependent mitophagy, and increases mitochondrial mass in cancer cells overexpressing AURKA. AURKA-IN-4 can be used in the research of breast cancer.

PROTAC AURKA degrader 1 is a AURKA PROTAC degrader. PROTAC AURKA degrader 1 forms a ternary complex with AURKA and CRBN E3 ligase, labels AURKA to induce its ubiquitination, and promotes its degradation via the ubiquitin-proteasome system. PROTAC AURKA degrader 1 is applicable to leukemia-related research.

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.

PROTAC AURKA degrader-4 is a AURKA PROTAC degrader with a DC₅₀ of 25.62 nM (Jurkat cells). PROTAC AURKA degrader-4 recruits the CRBN E3 ubiquitin ligase via the ubiquitin-proteasome system. PROTAC AURKA degrader-4 disrupts both the catalytic and non-catalytic functions of AURKA, including its interactions with TPX2 and c-Myc. PROTAC AURKA degrader-4 induces G2/M phase arrest and apoptosis. PROTAC AURKA degrader-4 exhibits enhanced antiproliferative activity and in vivo antitumor efficacy in models with high CRBN and AURKA expression. PROTAC AURKA degrader-4 can be used for the research of acute lymphoblastic leukemia.

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 Aurora A Degrader-1 is an orally active and blood-brain barrier-permeable selective Aurora A PROTAC degrader. PROTAC Aurora A Degrader-1 induces AURKA degradation with a DC₅₀ of 6 nM in IMR32 cells (D_max = 95%), eliminates both the kinase catalytic activity and N-Myc stabilizing scaffolding function of Aurora A, induces DNA damage, G2/M arrest and apoptosis, and shows antiproliferative activity. PROTAC Aurora A Degrader-1 is applicable to the research of neuroblastoma and small cell lung cancer.