2. Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation
  3. Histone Acetyltransferase Arginase
  4. Conophyllidine

Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs.

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

Conophyllidine

Conophyllidine Chemical Structure

CAS No. : 152406-44-5

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.

Conophyllidine Related Antibodies

Top Publications Citing Use of Products

View All Histone Acetyltransferase Isoform Specific Products:

View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs[1].

IC50 & Target[1]

CBP/p300

 

In Vitro

Conophyllidine (Compound CX-1) (0-1 μM, 12 h) selectively inhibits M2 polarization, without affecting M1 activation in macrophages[1].
Conophyllidine (50 μM, 12 h) targets P300/CBP and inhibits histone H3K27 acetylation in macrophages [1].

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

Conophyllidine Related Antibodies

Immunofluorescence[1]

Cell Line: Macrophages
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 12 h
Result: Suppressed IL-4 and induced CD206 expression.
Inhibited IL-4-induced expressions of Arg1, Chil3, Retnla, and Mgl2, as well as LPS-induced expressions of Arg1 and IL10.

Western Blot Analysis[1]

Cell Line: Macrophages
Concentration: 50 μM
Incubation Time: 12 h
Result: Did not affect the expression of P300/CBP.
Interacted with the full-length P300, the BD and HAT domains, and the HAT domain with PEG-biotin.
In Vivo

Conophyllidine (Compound CX-1) (2 mg/kg, i.p., once daily for 3 days) inhibits tumor progression and triggers tumor immunity of mice by reprogramming the TAMs in B16F10 melanoma and 4T1 breast cancer models[1].

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

Animal Model: B16F10 melanoma model established in C57BL/6J mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days
Result: Significantly delayed tumor growth, prolonged the survival of mice without body weight loss.
Induced upregulation of the macrophage population.
Inhibited the CD206 expression and elevated the MHCII expression.
Upregulated the population of tumor-infiltrating CD8+ T cells and did not affect the population of CD4+ T cells Elevated the expressions of IFNγ, GzmB, and TNFα.
Animal Model: 4T1 breast cancer model established in BALB/c or BALB/c nu/nu mice[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 3 days
Result: Inhibited lung metastasis of breast cancer.
Molecular Weight

778.89

Formula

C44H50N4O9
CAS No.
SMILES

CC[C@@]12[C@@]3([H])[C@]4(CCN3[C@@]5([H])[C@@](OC6=CC(NC7=C(C(OC)=O)C[C@@]8(CC)[C@@]9([H])[C@]7%10CCN9CC=C8)=C%10C=C65)([H])[C@H]2O)C(NC%11=C(OC)C(OC)=C(O)C=C%114)=C(C1)C(OC)=O
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.

Conophyllidine 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:

Conophyllidine152406-44-5Histone AcetyltransferaseArginaseHATsHATBisindoleCX-1Tumor-associated macrophagesCD8+Tumor immunityP300/CBPInhibitorinhibitorinhibit

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:
Conophyllidine
Cat. No.:
HY-175180
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.