2. Cell Cycle/DNA Damage NF-κB Apoptosis
  3. G-quadruplex Keap1-Nrf2 Ferroptosis Apoptosis
  4. Anticancer agent 309

Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer.

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

Anticancer agent 309

Anticancer agent 309 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.

Anticancer agent 309 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer[1].

In Vitro

Anticancer agent 309 binds potently to purified c-Myc G4 and KRAS G4 structures, with Kd values of 2.46 μM and 1.61 μM, respectively[1].
Anticancer agent 309 (24 h) inhibits the proliferation of various human and mouse tumor cell lines (MDA-MB-231, HCT116, HepG2, A549, MCF-7, 4T1), with IC50 values ranging from 7.77 ± 0.77 μM to 16.71 ± 0.71 μM[1].
Anticancer agent 309 (10 μM; 24 h) promotes the formation of nuclear G4 in human breast cancer MDA-MB-231 cells[1].
Anticancer agent 309 (5-20 μM; 24 h) triggers apoptosis in breast cancer MDA-MB-231 cells[1].

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

Anticancer agent 309 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human breast cancer MDA-MB-231 cells, human colon cancer HCT116 cells, human liver cancer HepG2 cells, human lung cancer A549 cells, human breast cancer MCF-7 cells, mouse breast cancer 4T1 cells, human normal breast MCF-10a cells
Concentration: Titrated to determine IC50
Incubation Time: 24 h
Result: Exerted dose-dependent cytotoxicity against all tested tumor cell lines, with IC50 values of 7.77 ± 0.77 μM (MDA-MB-231), 8.33 ± 0.46 μM (HCT116), 9.88 ± 1.18 μM (HepG2), 11.67 ± 0.33 μM (A549), 16.71 ± 0.71 μM (MCF-7), and 15.23 ± 0.95 μM (4T1).
Showed an IC50 of 28.12 ± 1.49 μM against normal MCF-10a cells, which was significantly higher than against tumor cells.

Western Blot Analysis[1]

Cell Line: Human breast cancer MDA-MB-231 cells
Concentration: 5-20 μM
Incubation Time: 24 h
Result: Downregulated c-Myc and KRAS protein expression in a dose-dependent manner.
Suppressed the NRF2 signaling pathway, reducing the expression of XCT and GPX4.
Decreased the expression of Caspase 7, Caspase 3, and anti-apoptotic Bcl-2, while increased Cleaved Caspase 3 expression at 20 μM.

Apoptosis Analysis[1]

Cell Line: Human breast cancer MDA-MB-231 cells
Concentration: 5-20 μM
Incubation Time: 24 h
Result: Triggered a dose-dependent increase in both early apoptotic and late apoptotic cell populations.
In Vivo

Anticancer agent 309 (10 mg/kg; once every other day; for 14 consecutive days) exerts potent antitumor effects on BALB/c mice bearing 4T1 breast cancer cells, while increasing the numbers of CD4+ and CD8+ T cells in the spleen and tumor[1].

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

Animal Model: BALB/c (female, 4 weeks old, subcutaneously inoculated with 4×105 4T1 mouse breast cancer cells)[1]
Dosage: 10 mg/kg
Administration: every other day; 14 days
Result: Reduced final tumor weight.
Suppressed tumor growth.
Elevated percentage of CD45+CD3+CD4+ helper T cells in spleens and in tumors.
Elevated percentage of CD45+CD3+CD8+ cytotoxic T lymphocytes in spleens and in tumors.
Induced downregulation of GPX4 and upregulation of Cleaved Caspase 3 in tumor tissues.
Did not cause significant mouse weight loss or major organ weight changes relative to controls.
Molecular Weight

492.66

Formula

C31H36N6
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)C3=C(NC(C4=CC=CC=C4)=N3)C5=CC=C(C=C5)N6CCN(CC6)C
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.

Anticancer agent 309 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:

Anticancer agent 309Anticancer agent309Anticancer agent-309G-quadruplexKeap1-Nrf2FerroptosisApoptosisferroptosisparallel G-quadruplexesimmunogenic cell deathc-Myc G-quadruplexCD4+ helper T lymphocytesNRF2-XCT-GPX4 pathwayapoptosisbreast cancer cellsKRAS G-quadruplexCD8+ cytotoxic T lymphocytesInhibitorinhibitorinhibit

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:
Anticancer agent 309
Cat. No.:
HY-182055
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.