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Pathways Recommended: PROTAC
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AURKA PROTAC degrader

" in MedChemExpress (MCE) Product Catalog:

16

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-11103
    Sitaxsentan sodium
    2 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan sodium
  • HY-171767
    SK2188

    JB325

    		 PROTACs Apoptosis Caspase Aurora Kinase Cancer
    SK2188 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 (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: Thalidomide (HY-14658); Black: Linker: Amino-PEG4-alcohol (HY-W008005)) .
    SK2188
  • HY-148065
    FMF-06-098-1

    		PROTACs Wee1 CDK AAK1 ULK MELK Itk IRAK Ephrin Receptor FGFR MAP4K p38 MAPK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
    FMF-06-098-1
  • HY-168543
    PROTAC MPS1 degrader 2

    		PROTACs Aurora Kinase Mps1 Cancer
    PROTAC MPS1 degrader 2 (Compound 15) is a potent degrader of monopolar spindle 1 (Mps1，TTK)，AURKA and AURKB，with DC50s of 42.0，2.1 and 154.0 nM，respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168545); Black: linker (HY-N0420); Blue: ligand for E3 ligase (HY-10984) .
    PROTAC MPS1 degrader 2
  • HY-137344A
    dAURK-4 hydrochloride

    		PROTACs Aurora Kinase Cancer
    dAURK-4 hydrochloride, an Alisertib (HY-10971) derivative, is a potent and selective PROTAC AURKA (Aurora A) degrader. dAURK-4 hydrochloride has anticancer effects. (Pink: Ligand for target protein (HY-10971); Black: Linker (HY-W004640); Blue: Ligand for E3 ligase Thalidomide-O-COOH (HY-103597)) .
    dAURK-4 hydrochloride
  • HY-171768
    SK2187

    JB301

    		 PROTACs Aurora Kinase Neurological Disease Cancer
    SK2187 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 (Pink: AURKA ligand: MK-5108 (HY-13252); Blue: E3 ligand (HY-103597); Black: Linker: Amino-PEG3-alcohol (HY-W015088)) .
    SK2187
  • HY-175830
    PROTAC AURKA degrader 1

    		PROTACs Aurora Kinase Cancer
    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)
    PROTAC AURKA degrader 1
  • HY-168540
    PROTAC MPS1 degrader 1

    		PROTACs Mps1 Aurora Kinase Cancer
    PROTAC MPS1 degrader 1 (Compound 19) is a potent degrader of monopolar spindle 1 (Mps1, TTK), AURKA and AURKB, with DC50s of 17.7, 108.7 and 570.3 nM, respectively. PROTAC MPS1 degrader 1 can be used for the research of acute myeloid leukemia. (Pink: ligand for target protein (HY-168542); Black: linker (HY-W141926); Blue: ligand for E3 ligase (HY-10984) .
    PROTAC MPS1 degrader 1
  • HY-175525
    MS44

    		PROTACs Aurora Kinase Cancer
    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 (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938)) .
    MS44
  • HY-175827
    MK-5108-NH-PEG2-alkyne

    		Aurora Kinase Ligands for Target Protein for PROTAC Cancer
    MK-5108-NH-PEG2-alkyne is a Aurora kinase A (AURKA) inhibitor. MK-5108-NH-PEG2-alkyne can be used for synthesis of PROTAC AURKA degrader 1 (HY-175830) .
    MK-5108-NH-PEG2-alkyne
  • HY-180132
    PROTAC AURKA degrader 2

    		PROTACs Aurora Kinase 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 .
    PROTAC AURKA degrader 2
  • HY-179641
    SK5527

    		PROTACs Aurora Kinase Cancer
    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 .
    SK5527
  • HY-179640
    SK4454

    		PROTACs Aurora Kinase Cancer
    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 .
    SK4454
  • HY-181568
    PROTAC Aurora A Degrader-1

    		PROTACs Aurora Kinase DNA/RNA Synthesis Apoptosis Neurological Disease 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 .
    PROTAC Aurora A Degrader-1
  • HY-181311
    CCT400028

    		PROTACs Aurora Kinase E1/E2/E3 Enzyme Neurological Disease Cancer
    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 KD 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 .
    CCT400028
  • HY-183098
    UNC8209

    		PROTACs IKK Apoptosis Cancer
    UNC8209 is a selective PROTAC-based TANK-binding kinase 1 (TBK1) degrader. UNC8209 recruits cereblon (CRBN) to mediate ubiquitin-proteasome pathway-dependent TBK1 degradation and reduces AAK1, GAK, and AURKA abundance. UNC8209 suppresses tumor cell proliferation, impairs in vivo tumor growth, inhibits colony and clonogenic growth and enhances tumor cell sensitivity to TNFα or IFN-γ. UNC8209 modulates cell cycle and induces mild apoptosis. UNC8209 can be used for the research of clear cell renal cell carcinoma, non-small cell lung cancer, pancreatic ductal adenocarcinoma .
    UNC8209

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