1. Apoptosis
  2. Ferroptosis
  3. FA16

FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc-), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model.

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

FA16 Chemical Structure

FA16 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FA16 is a specific ferroptosis inducer (IC50=1.26 μM; HT1080 cells) with metabolic stability, is the derivate of 2-(trifluoromethyl)benzimidazole. FA16 acts by inhibiting cystine/glutamate antiporter (system Xc-), which mediates the exchange of intracellular glutamate and extracellular cystine. FA16 significantly inhibits tumor growth in the HepG2 xenograft model[1].

In Vitro

FA16 (1 μM; 5 min) has satisfactory metabolic stability in rat and human liver microsomes[1].
FA16 (5 μM; 10 h) induces lipid ROS accumulation and inhibits glutamate release dose-dependently in HT1080 cells[1].
FA16 (5 μM; 24 h) results mitochondria shrunken with increased membrane density, which was in line with the morphological feature related to ferroptosis[1].
FA16 (10 μM; 24 h) induced cell death, which can be rescued by the ferroptosis inhibitors Fer-1, Trolox or DFO, but not by the inhibitors of apoptosis or necroptosis[1].

Parameter Microsomal stability (T1/2 min) Intrinsic clearance (μL/min/ mg protein)
Human 15.6 88.6
Rat 10.4 132.8

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

Cell Viability Assay[1]

Cell Line: Human cancer cell lines: Clear-cell renal cell carcinoma cells (786-O), breast cancer cells (MDA-MB-231), cervical cancer cells (HeLa), hepatocellular carcinoma cells (HepG2), melanoma cells (A375), and prostate cancer cells (DU145); Human normal cell lines: cardiomyocytes (AC16), colon mucosal epithelial cells (NCM460), embryonic kidney cells (293T), and hepatic cells (LO2)
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Inhibited cell growth with IC50s of 0.7 μM (786-O), 4.34 μM (MDA-MB-231), 1.91 μM (HeLa), 1.33 μM (HepG2), 2.31 μM (A375), and 1.64 μM (DU145), respectively.

Immunofluorescence[1]

Cell Line: HT1080 cells
Concentration: 5 μM
Incubation Time: 10 hours
Result: Significantly induced lipid ROS accumulation, as indicated by the great enhancement in green fluorescence intensity.

RT-PCR[1]

Cell Line: HT1080 cells
Concentration: 0.5 μM, 1 μM, and 5 μM
Incubation Time: 6 hours and 18 hours
Result: Increased the system Xc- component SLC7A11, ChaC GSHspecific γ-glutamylcyclotransferase 1 (CHAC1), but little changed GPX4.
In Vivo

FA16 (15 or 30 mg/kg; i.p.; every other for 21 d) significantly inhibits tumor growth with good safety (no weight loss) in 786-O xenograft mice model, and it induced ferroptosis in tumor tissues[1].

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

Animal Model: BALB/c nude mice bearing HepG2 tumors (s.c.)[1]
Dosage: 15 or 30 mg/kg
Administration: Intraperitoneal injection; every other for 21 days
Result: Significantly inhibited tumor growth with a tumor growth inhibition (TGI) value of 47.6% and 77.1% at 15 and 30 mg/ kg, respectively.
Molecular Weight

466.52

Formula

C22H25F3N4O2S

SMILES

CN(S(=O)(C1=CC=C(C=C1)N2CCC(CC2)CN3C4=CC=CC=C4N=C3C(F)(F)F)=O)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.

FA16 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
FA16
Cat. No.:
HY-151964
Quantity:
MCE Japan Authorized Agent: