2. PROTAC Neuronal Signaling GPCR/G Protein PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis
  4. 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. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)).

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

PROTAC CB1R Degrader-1

PROTAC CB1R Degrader-1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC CB1R Degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Cannabinoid Receptor Isoform Specific Products:

View All Isoforms
CB1 CB2

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

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.

PROTAC CB1R Degrader-1 Related Antibodies

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.
Molecular Weight

761.01

Formula

C35H28Cl3N9O5
SMILES

ClC(C=C1)=CC=C1C(N(N=C2C(NCC3=CN(N=N3)CCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC CB1R Degrader-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC CB1R Degrader-1PROTACsCannabinoid ReceptorAktERKBcl-2 FamilyApoptosisPKBProtein kinase BExtracellular signal regulated kinasesCB1RUPSMCF-7p-AKTp-ERKBCL2MCM5apoptosisPROTACbreast cancerMDA-MB-231Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC CB1R Degrader-1
Cat. No.:
HY-178176
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.