PROTAC CB1R Degrader-1
PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research.
(Pink: ligand (HY-134497); Blue: Cereblon ligand (HY-41547); Black: linker (HY-178198)).
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- 화학식: C35H28Cl3N9O5
- 분자량:761.01
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보관:
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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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
More
Biological Activity
제품 설명
IC50 & Target
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CB1R |
Cereblon |
In Vitro
PROTAC CB1R Degrader-1 (Pro-CB8) (0.1-20 μM, 6-48 h) induces significant, dose- and time-dependent degradation of CB1R in MCF-7 cells (DC50 = 3.37 μM), with a substantial reduction also observed in MDA-MB-231 cells, supporting its broader applicability[1].
PROTAC CB1R Degrader-1 (0-10 μM, 6-48 h) downregulates key cancer-related proteins (p-AKT, p-ERK) and genes (BCL2, MCM5) in breast cancer cells, including MCF-7 and MDA-MB-231 cells[1].
PROTAC CB1R Degrader-1 (0-10 μM, 48 h) selectively decreases viability and proliferation in breast cancer cells (MCF-7 and MDA-MB-231) while sparing healthy fibroblasts, and induces significant apoptosis in both cancer cell lines (MCF-7 and MDA-MB-231)[1].
PROTAC CB1R Degrader-1 (10 μM) results in pronounced and sustained disintegration of both MCF-7 and MDA-MB-231 spheroids in 3D experimental models, beginning as early as day 3 and persisting throughout the observation period[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Significantly reduced CB1R levels by approximately 80% at 10 μM.
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Cell Line:MCF-7 cells
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Concentration:1, 2, 5, 10, and 20 μM
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Incubation Time:6, 12, 24, and 48 h
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Result:Reduced CB1R levels in a time-dependent manner, with the most potent effect observed after 48 h.
significantly reduced CB1R protein levels, achieving approximately 75% degradation at 20 μM with a calculated degradation concentration (DC50 = 3.37 μM).
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Cell Line:MDA-MB-231 cells
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Concentration:0.1, 1, and 10 μM
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Incubation Time:48 h
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Result:Induced a significant reduction in CB1R levels, with a maximum decrease of approximately 90% at 10 μM.
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Cell Line:MCF-7 cells
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Concentration:10 μM
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Incubation Time:6, 12, 24 and 48 h
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Result:Markedly decreased levels of p-AKT and p-ERK by approximately 70%.
Decreased BAL2 levels in a time-dependent manner at 10 μM, with a 56% reduction after 48 h.
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Cell Line:MCF-7 cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Decreased MCM5 and BCL2 mRNA levels at 1 and 10 μM.
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Cell Line:MCF-7 and fibroblast cells
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Concentration:0.1, 1, and 10 μM
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Incubation Time:48 h
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Result:Decreased cell viability at 0.1, 1, and 10 μM in MCF-7 cells.
Showed no significant effect on fibroblast cells.
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Cell Line:MCF-7 and MDA-MB-231 cells
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Concentration:0, 1, and 10 μM for MCF-7 cells; 0, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
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Incubation Time:48 h
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Result:Decreased MCF-7 cell proliferation at 1, and 10 μM.
Decreased MDA-MB-231 cell proliferation at 1 and 10 μM.
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Cell Line:MCF-7 and MDA-MB-231 cells
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Concentration:10 μM for MCF-7 cells, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
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Incubation Time:48 h
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Result:Resulted in a robust increase in apoptosis at 10 μM in MCF-7 cells.
Induced a dose-dependent marked increase in apoptosis in MDA-MB-231 cells at 1 and 10 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- 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
- Breast Cancer Modeling
- 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
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- MTT Cell Proliferation Assay
Chemical Information
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분자량 761.01
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화학식 C35H28Cl3N9O5
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SMILES
ClC(C=C1)=CC=C1C(N(N=C2C(NCCN3N=NC(CNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=C3)=O)C7=CC=C(C=C7Cl)Cl)=C2C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC CB1R Degrader-1 Related Classifications
HY-178176 Related Classifications
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