eEF2K Degrader-3
eEF2K Degrader-3 is an eEF2K molecular glue degrader (Kd = 0.831 μM) that recruits βTRCP to mediate ubiquitin-proteasome degradation. eEF2K Degrader-3 triggers rapid downregulation of eEF2K and produces a durable effect. eEF2K Degrader-3 inhibits TNBC cell proliferation, migration, and invasion, suppresses tumor growth and lung metastasis in mouse models, decreases vimentin and increases E-cadherin in organoids, and downregulates AURKA and SOX8 downstream of eEF2K degradation. eEF2K Degrader-3 can be used for research on triple-negative breast cancer (TNBC).
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- CAS No.: 1043812-24-3
- Formule: C28H32N4O5
- Masse moléculaire:504.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
CaMK III/eEF-2K 0.831 μM (Kd) |
In Vitro
eEF2K Degrader-3 (0-3.2 μM; 4 days) exerts anticancer activity in TNBC PDOs, reducing organoid growth and downregulating eEF2K/AURKA/SOX8 signaling[1].
eEF2K Degrader-3 (0.2 μM; 30 min) binds to eEF2K in MDA-MB-231 cells[1].
eEF2K Degrader-3 (10 μM) binding to eEF2K depends on residues R140, V168, R144, and Y236, whereas C146 is not required[1].
eEF2K Degrader-3 (0.1-0.4 μM) promotes the recruitment of βTRCP to eEF2K and increases ubiquitination of eEF2K in HEK293T cells; it degrades eEF2K and reduces AURKA and SOX8 protein levels in MDA-MB-231 and HCC1806 cells without affecting eEF2K mRNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TNBC organoids
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Concentration:0.2, 0.4, 0.8, 1.6, 3.2 μM
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Incubation Time:4 days
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Result:Reduced organoid growth.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (2 ×106 MDA-MB-231 cell lines were subcutaneously injected into the
right flank)[1] -
Dosage:5, 10 mg/kg
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Administration:intraperitoneal injection every other day; for 18 days
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Result:Inhibited tumor growth and lung metastasis in MDA‑MB‑231 xenograft nude mice, with no obvious hepatorenal toxicity and no body weight loss in mice.
- BrdU Incorporation Assay
- Cell migration
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Tail-Vein Experimental Metastasis Xenograft
- Cell invasion
- MTT Cell Proliferation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 1043812-24-3
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Masse moléculaire 504.58
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Formule C28H32N4O5
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SMILES
O=C(C1CN(C(C2=NN(C3=CC=C(C)C(C)=C3)C(N(CC4=CC=CC(C)=C4)C2=O)=O)=O)CCC1)OCC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
eEF2K Degrader-3 Related Classifications
HY-190183 Related Classifications
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