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Cat. No.: HY-178176

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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: CB1R ligand (HY-134497); Blue: Cereblon ligand (HY-41547); Black: linker (HY-178198)).

For research use only. We do not sell to patients.

Formula: C₃₅H₂₈Cl₃N₉O₅
Molecular Weight:761.01

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (279 KB)

PROTAC CB1R Degrader-1 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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^[1]. (Pink: CB1R ligand (HY-134497); Blue: Cereblon ligand (HY-41547); Black: linker (HY-178198)).

IC₅₀ & Target

CB1R

Cereblon

All PROTACs Isoforms :

All Cannabinoid Receptor Isoforms :

All Akt Isoforms :

All ERK Isoforms :

All Bcl-2 Family Isoforms :

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.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

10 μM
Incubation Time:

48 h
Result:

Significantly reduced CB1R levels by approximately 80% at 10 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

1, 2, 5, 10, and 20 μM
Incubation Time:

6, 12, 24, and 48 h
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).

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0.1, 1, and 10 μM
Incubation Time:

48 h
Result:

Induced a significant reduction in CB1R levels, with a maximum decrease of approximately 90% at 10 μM.

Western Blot Analysis^[1]

Cell Line:

MCF-7 cells
Concentration:

10 μM
Incubation Time:

6, 12, 24 and 48 h
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.

Real Time qPCR^[1]

Cell Line:

MCF-7 cells
Concentration:

0.1, 1 and 10 μM
Incubation Time:

24 h
Result:

Decreased MCM5 and BCL2 mRNA levels at 1 and 10 μM.

Cell Viability Assay^[1]

Cell Line:

MCF-7 and fibroblast cells
Concentration:

0.1, 1, and 10 μM
Incubation Time:

48 h
Result:

Decreased cell viability at 0.1, 1, and 10 μM in MCF-7 cells.
Showed no significant effect on fibroblast cells.

Cell Proliferation Assay^[1]

Cell Line:

MCF-7 and MDA-MB-231 cells
Concentration:

0, 1, and 10 μM for MCF-7 cells; 0, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
Incubation Time:

48 h
Result:

Decreased MCF-7 cell proliferation at 1, and 10 μM.
Decreased MDA-MB-231 cell proliferation at 1 and 10 μM.

Apoptosis Analysis^[1]

Cell Line:

MCF-7 and MDA-MB-231 cells
Concentration:

10 μM for MCF-7 cells, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
Incubation Time:

48 h
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

PROTAC CB1R Degrader-1 (5 mg/kg, i.p., once) exhibits minimal brain penetration and is unlikely to cross the blood-brain-barrier in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 761.01
Formula C₃₅H₂₈Cl₃N₉O₅
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kashkush A, et al. Development of PROTAC-Based Strategies for Cannabinoid Receptor Type 1 (CB1R) Degradation in Cancer. ACS Pharmacol Transl Sci. 2025 Sep 3;8(9):3160-3169. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC CB1R Degrader-1

All PROTACs Isoforms

All Cannabinoid Receptor Isoforms

All Akt Isoforms

All ERK Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC CB1R Degrader-1 Related Classifications

HY-178176 Related Classifications