PROTAC PLK1 Degrader-2
Based on 1 Customer Validation
PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC. PROTAC PLK1 Degrader-2 utilizes Arg12 as dual-function cell-permeable N-degron to recruit UBR1/UBR2 E3 ligases, mediates PLK1 ubiquitination and proteasome-dependent degradation. PROTAC PLK1 Degrader-2 suppresses cervical cancer cell proliferation, induces G2/M cell cycle arrest and tumor cell apoptosis, and exerts potent in vivo anti-tumor efficacy in mice and can be applied to research on PLK1-driven cervical carcinoma (PLK1 ligand: POI ligand-3 (HY-180990); E3 ligase ligand: Arg12 (HY-P11631); PROTAC linker: 6-Aminocaproic acid (HY-B0236)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.48%
- Formel: C116H216N57O23P
- Molecular Weight:2808.30
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PLK1 6.06 μM (IC50) |
In Vitro
PROTAC PLK1 Degrader-2 (compound NC1) (1-5 μM; 24 h) induces dose-dependent degradation of endogenous PLK1 protein in HeLa cervical cancer cells[1].
PROTAC PLK1 Degrader-2 (5 μM; 24 h) completely loses PLK degradation activity after co-treatment with proteasome inhibitor MG-132 (HY-13259)[1].
PROTAC PLK1 Degrader-2 (6 μM; 24 h) induces G2/M phase cell cycle arrest in HeLa cells and effectively penetrates HeLa cell membrane and accumulates in cell nucleus[1].
PROTAC PLK1 Degrader-2 (0.325-12 μM; 24 h) suppresses HeLa cell viability in a concentration-dependent manner with cell proliferation IC50 = 5.23 μM[1].
PROTAC PLK1 Degrader-2 binds recombinant PLK1 PBD protein with a dissociation constant Kd = 6.06 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa
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Concentration:1, 2, 3, 4, 5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent PLK1 degradation in HeLa cells with a DC50 of 2.06 μM.
Rescued PLK1 protein levels when combined with the proteasome inhibitor MG-132.
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Cell Line:HeLa
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Concentration:0.325, 0.75, 1.5, 3, 6, 12 μM
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Incubation Time:24 h
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Result:Inhibited HeLa cell proliferation with an IC50 of 5.23 μM.
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Cell Line:HeLa
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Concentration:6 μM
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Incubation Time:24 h
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Result:Induced G2/M phase cell cycle arrest.
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Cell Line:HeLa
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Concentration:6 μM
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Incubation Time:24 h
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Result:Induced apoptosis in HeLa cells, with early apoptosis at 13.27% and late apoptosis at 19.59%.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Subcutaneous xenograft nude mouse model of human HeLa cervical cancer[1]
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Dosage:4 mg/kg
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Administration:tail vein injection, every 3-4 days for 29 days
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Result:Inhibited tumor volume growth.
Showed no obvious mouse body weight loss.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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Appearance Solid
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Molecular Weight 2808.30
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Formel C116H216N57O23P
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Color White to off-white
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Sequence
Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-{Ahx}-Pro-Leu-{His(n-octylphenyl )}-Ser-{pThr}-NH2
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Sequence Shortening
RRRRRRRRRRRR-{Ahx}-PL-{His(n-octylphenyl )}-S-{pThr}-NH2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 3.33 mg/mL (1.19 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Reinheit & Dokumentation
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Data Sheet (293 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.3561 mL | 1.7804 mL | 3.5609 mL | 8.9022 mL |
PROTAC PLK1 Degrader-2 Related Classifications
HY-180989 Related Classifications
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