2. Immunology/Inflammation Apoptosis
  3. PD-1/PD-L1 Bcl-2 Family MDM-2/p53 Caspase
  4. CSN5-IN-3

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.

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

CSN5-IN-3

CSN5-IN-3 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.

CSN5-IN-3 Related Antibodies

Top Publications Citing Use of Products

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 Bad

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer[1].

IC50 & Target[1]

Caspase 3

 

Bcl-2

 

CSN5

0.58 μM (IC50)

In Vitro

CSN5-IN-3 (20 min) acts as a potent CSN5 inhibitor in cell-free fluorescence polarization assays, with an IC50 of 0.58 μM[1].
CSN5-IN-3 (72 h) potently inhibits the viability of MDA-MB-231 cells, with an IC50 value of 2.1 μM[1].

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

CSN5-IN-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 2.5-20 μM (direct treatment); 10 μM (following 2 h preincubation with MG132 or MLN4924)
Incubation Time: 12 h
Result: Dose-dependently increased NEDD8-Cul1 protein levels while not altering CSN5 expression.
Dose-dependently reduced PD-L1 protein levels.
Dose-dependently upregulated P53, and cleaved caspase-3 protein levels.
Dose-dependently downregulated Bcl-2 protein levels.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Caused no significant change in G0/G1 phase cell percentage at 1 μM.
Increased G0/G1 phase cell percentage by 9.6% compared to control at 5 μM (p < 0.01).
Increased G0/G1 phase cell percentage by 18.3% compared to control at 10 μM (p < 0.001).
In Vivo

CSN5-IN-3 (8-16 mg/kg; i.p.; once every 3 days; for 21 consecutive days) exerts potent, dose-dependent in vivo anti-tumor activity against MDA-MB-231 xenografts in mice[1].

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

Animal Model: BALB/c nude (female, 4 weeks old, triple-negative breast cancer subcutaneous xenograft model)[1]
Dosage: 8 mg/kg; 16 mg/kg
Administration: i.p.; every 3 days; 21 days
Result: Achieved 68.3% tumor growth inhibition (TGI) at 8 mg/kg.
Achieved 89.3% tumor growth inhibition (TGI) at 16 mg/kg.
Showed no mortality in either treatment group.
Exhibited no significant body weight changes in the low-dose group; caused a slight temporary body weight decrease but no significant end-of-study weight loss in the high-dose group.
Reduced PD-L1 and Ki67 expression, and increased P21 expression in excised tumors via immunohistochemical analysis.
Molecular Weight

441.57

Formula

C27H31N5O
SMILES

CC1=CC=C(C(C2=CC(OC)=CC=C2)=C1)C3=CC4=C(N3)N=CC=C4NCCN5CCNCC5
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.

CSN5-IN-3 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:

CSN5-IN-3PD-1/PD-L1Bcl-2 FamilyMDM-2/p53CaspasePD-1/Programmed death-ligand 1NEDD8-Cul1Bcl-2CSN5P27P53/Bax-dependent apoptosisPD-L1MDA-MB-231 cellstriple-negative breast cancerG0/G1 cell cycle arrestP21Inhibitorinhibitorinhibit

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:
CSN5-IN-3
Cat. No.:
HY-181795
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.