2. Apoptosis
  3. Transferrin Receptor Ferroptosis Apoptosis Necroptosis
  4. TfR-1-IN-1

TfR-1-IN-1 is a transferrin receptor-1 (TfR-1) inhibitor with tumor cell-specific activity. TfR-1-IN-1 reduces TfR-1 expression, impairs mitochondrial function, induces cell apoptosis, necroptosis and ferroptosis, and increases intracellular iron (II) levels. TfR-1-IN-1 decreases the metabolic activity of cancer cells. TfR-1-IN-1 can be used for the research of ovarian cancer, breast cancer and acute myeloid leukemia.

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

TfR-1-IN-1

TfR-1-IN-1 Chemical Structure

CAS No. : 1643444-62-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

TfR-1-IN-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TfR-1-IN-1

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Description

TfR-1-IN-1 is a transferrin receptor-1 (TfR-1) inhibitor with tumor cell-specific activity. TfR-1-IN-1 reduces TfR-1 expression, impairs mitochondrial function, induces cell apoptosis, necroptosis and ferroptosis, and increases intracellular iron (II) levels. TfR-1-IN-1 decreases the metabolic activity of cancer cells. TfR-1-IN-1 can be used for the research of ovarian cancer, breast cancer and acute myeloid leukemia[1].

IC50 & Target[1]

TfR-1

 

In Vitro

TfR-1-IN-1 (C4) (0.1-10 μM; 72 h) potently reduces the metabolic activity of MDA-MB 231, HL-60 and A2780cis tumor cells, with IC50 values of 0.46, 0.48 and 0.51 μM, respectively; it also exhibits tumor cell specificity at a concentration of 0.5 μM and shows no effect on non-malignant HS-5 cells[1].
TfR-1-IN-1 (1 μM; 2-24 h) increases intracellular iron levels in MDA-MB 231 cells, with the level rising from 69.7 pg Fe/μg protein at 12 h to 86.0 pg Fe/μg protein at 24 h[1].
TfR-1-IN-1 (0.1-1 μM; 12-24 h) downregulates TfR-1 expression in MDA-MB 231 cells in a concentration- and time-dependent manner[1].
TfR-1-IN-1 (1 μM; 4-20 h) significantly increases the labile iron 2+ pool in MDA-MB 231 cells within 4 h, while ferristatin II-mediated inhibition of TfR-1 partially attenuates this effect[1].
TfR-1-IN-1 (0.1-0.5 μM; 24 h) reduces the mitochondrial membrane potential of MDA-MB 231 cells in a concentration-dependent manner, and treatment with 0.5 μM for 24 h decreases ΔΨm to 57.3% of that in the control group[1].
TfR-1-IN-1 (1 μM; 24 h) induces cell death in MDA-MB 231 cells, with apoptotic death accounting for 25.9% and non-apoptotic death accounting for 49.8%[1].
TfR-1-IN-1 (0.1-1 μM; 2-4 h) induces concentration-dependent lipid peroxidation in MDA-MB 231 cells, with a peroxidation level of 3.5% observed after treatment with 1 μM for 4 h, whereas non-malignant HS-5 cells show only an extremely weak response[1].

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

TfR-1-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB 231, HL-60, and A2780cis tumor cells, HS-5 cells
Concentration: 0.1, 0.25, 0.5, 1, 10 μM
Incubation Time: 72 h
Result: Reduced metabolic activity in a concentration-dependent manner across all tumor cell lines.
Reduced metabolic activity in MDA-MB 231 cells with an IC50 of 0.46 μM.
Reduced metabolic activity in HL-60 cells with an IC50 of 0.48 μM.
Reduced metabolic activity in A2780cis cells with an IC50 of 0.51 μM.
Reduced metabolic activity in A2780 cells with an IC50 of 1.79 μM.
Showed no reduction in metabolic activity in HS-5 cells at 0.5 μM.
Inhibited HS-5 cell metabolic activity to 56.2% at 1 μM.
Reduced HS-5 cell metabolic activity to <10% at 10 μM.

Western Blot Analysis[1]

Cell Line: MDA-MB 231 breast cancer cells
Concentration: 0.1 μM, 1 μM
Incubation Time: 12, 24 h
Result: Reduced TfR-1 expression to 69.2% of untreated cells at 0.1 μM after 12 h.
Reduced TfR-1 expression to 38.4% of untreated cells at 0.1 μM after 24 h.
Reduced TfR-1 expression to 51.8% of untreated cells at 1 μM after 12 h.
Reduced TfR-1 expression to 33.7% of untreated cells at 1 μM after 24 h.
Exerted a greater 12 h effect on TfR-1 expression than 1 μM FeCl3 (61.1% expression).

Apoptosis Analysis[1]

Cell Line: MDA-MB 231 breast cancer cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Increased apoptotic cell death to 25.9% compared to untreated cells (13.5% apoptotic).
Increased nonapoptotic cell death to 49.8% compared to untreated cells (15.9% nonapoptotic dead cells).
Molecular Weight

441.62

Formula

C20H12ClF2FeN2O2
CAS No.
Appearance

Solid

Color

Brown to black

SMILES

FC1=CC=CC2=C1C=[N]3C4=CC=CC=C4[N]5=CC6=C(F)C=CC=C6[O-][Fe+3]5([Cl-])3[O-]2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (45.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2644 mL 11.3220 mL 22.6439 mL
5 mM 0.4529 mL 2.2644 mL 4.5288 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2644 mL 11.3220 mL 22.6439 mL 56.6098 mL
5 mM 0.4529 mL 2.2644 mL 4.5288 mL 11.3220 mL
10 mM 0.2264 mL 1.1322 mL 2.2644 mL 5.6610 mL
15 mM 0.1510 mL 0.7548 mL 1.5096 mL 3.7740 mL
20 mM 0.1132 mL 0.5661 mL 1.1322 mL 2.8305 mL
25 mM 0.0906 mL 0.4529 mL 0.9058 mL 2.2644 mL
30 mM 0.0755 mL 0.3774 mL 0.7548 mL 1.8870 mL
40 mM 0.0566 mL 0.2830 mL 0.5661 mL 1.4152 mL
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TfR-1-IN-1 Related Classifications

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:

TfR-1-IN-11643444-62-5Transferrin ReceptorFerroptosisApoptosisNecroptosisTfRCD71breast cancerMDA-MB 231acute myeloid leukemiaHL-60apoptosismitochondrial functionnecroptosisovarian cancerferroptosisTransferrin receptor-1Inhibitorinhibitorinhibit

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