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Art. -Nr.: HY-183364

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MTHFD2-IN-8

MTHFD2-IN-8 is a selective MTHFD2 inhibitor with an IC₅₀ of 0.066 μM. MTHFD2-IN-8 directly binds to intracellular mitochondrially localized protein MTHFD2 and accumulates selectively in tumor mitochondria. MTHFD2-IN-8 increases intracellular ROS levels, induces mitochondrial membrane potential depolarization, arrests cell cycle at G0/G1 phase, promotes apoptosis in cancer cells. MTHFD2-IN-8 inhibits tumor growth in a mouse colon cancer graft model.

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Formel: C₄₁H₄₀BrO₅P
Molecular Weight:723.63

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MTHFD2-IN-8 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

MTHFD2

0.066 μM (IC₅₀)

In Vitro

MTHFD2-IN-8 (Compound 2c) (1.5625-100 μM; 48 h) potently inhibits viability of A549, HCT116, SW620, and CT26 tumor cells with IC₅₀ values ranging from 5.17 μM to 9.72 μM, and exhibits selective toxicity against tumor cells over normal HEK293 cells (IC₅₀ = 17.69 μM)^[1].
MTHFD2-IN-8 (5 μM; 10 h) selectively accumulates in HCT116 colon tumor cell mitochondria, reaching levels 9.16-fold higher than in normal HEK293 cell mitochondriaa^[1].
MTHFD2-IN-8 (2.5-10 μM; 24 h) induces concentration-dependent apoptosis in HCT116 colon tumor cells^[1].
MTHFD2-IN-8 (2.5-10 μM; 24 h) induces concentration-dependent G0/G1 cell cycle arrest in HCT116 colon tumor cells^[1].
MTHFD2-IN-8 (2.5-10 μM; 24 h) induces concentration-dependent mitochondrial membrane potential depolarization and increases in intracellular ROS levels in HCT116 colon tumor cells^[1].
MTHFD2-IN-8 potently and selectively inhibits purified MTHFD2 enzymatic activity with an IC₅₀ of 0.066 μM, showing 43.78-fold higher selectivity for MTHFD2 over MTHFD1 (IC₅₀ = 2.89 μM)^[1].
MTHFD2-IN-8 (10 μM; 48 h) inhibits HCT116 colon tumor cell proliferation by targeting MTHFD2-mediated one-carbon metabolism, as shown by partial reversal of antiproliferative activity with Sodium formate (HY-W088065) supplementation^[1].
MTHFD2-IN-8 (3 h) directly binds to intracellular MTHFD2 in HCT116 colon tumor cells, increasing the protein's thermal stability^[1].

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

Cell Viability Assay^[1]

Cell Line:

A549, HCT116, SW620, CT26, HEK293 cells
Concentration:

1.5625,
3.125, 6.25, 12.5, 25, 50, 100 μM
Incubation Time:

48 h
Result:

Potently inhibited viability of all tested tumor cell lines: A549 with an IC₅₀ of 6.86 μM, HCT116 with an IC₅₀ of 5.17 μM, SW620 with an IC₅₀ of 7.84 μM, and CT26 with an IC₅₀ of 9.72 μM.
Inhibited normal HEK293 cell viability with an IC₅₀ of 17.69 μM, resulting in a selectivity index (SI, IC₅₀ HEK293/IC₅₀ HCT116) of ≈3.42.

Apoptosis Analysis^[1]

Cell Line:

HCT116
Concentration:

2.5, 5, 10 μM
Incubation Time:

24 h
Result:

Increased cell loss and induced apoptotic nuclear changes (intense blue fluorescence, crescent-shaped bands, discrete foci) in a concentration-dependent manner.\nIncreased total apoptotic cell proportion in a concentration-dependent manner: from 7.11% in the control group to 17.03% (2.5 μM), 21.89% (5 μM), and 30.2% (10 μM).
Increased the proportion of necrotic cells.

Cell Cycle Analysis^[1]

Cell Line:

HCT116
Concentration:

2.5, 5, 10 μM
Incubation Time:

24 h
Result:

Increased the proportion of cells in the G0/G1 phase in a concentration-dependent manner: from 45.6% in the control group to 50.3% (2.5 μM), 57.2% (5 μM), and 62.6% (10 μM).

In Vivo

MTHFD2-IN-8 (Compound 2c) (20-40 mg/kg; i.p.; once every 3 days; 2 weeks) inhibits colon cancer growth in a dose-dependent manner in a mouse subcutaneous graft model, achieving a 62.64% tumor inhibition rate at 40 mg/kg, with no observed in vivo toxicity to major organs^[1].

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

Animal Model:

Colon cancer BALB/c mice (male, 6-8 weeks old, subcutaneous graft model via injection of 1×10⁶ CT26 cells)^[1]
Dosage:

20 mg/kg; 40 mg/kg
Administration:

i.p.; once every 3 days; 2 weeks
Result:

Achieved a 49.70% tumor inhibition rate at 20 mg/kg.
Achieved a 62.64% tumor inhibition rate at 40 mg/kg.
Significantly decreased tumor growth curves compared with the control group.
Maintained stable body weight during treatment.
Showed no obvious abnormalities in major organs (myocardial fibers, hepatocytes, splenic lymphocytes, renal cells, alveolar structures) with no signs of degeneration, necrosis, inflammatory infiltration, or disorganized tissue structure.

Chemical Information

Molecular Weight 723.63
Formel C₄₁H₄₀BrO₅P
SMILES

O=C(C=C(C1=CC=CC=C1)O2)C(C2=C3)=C(O)C(O)=C3OCCCCCCCC[P+](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6.[Br-]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Hong A, et al. Discovery and in vitro and in vivo activity evaluation of novel baicalein phosphonium salt derivatives targeting mitochondrial MTHFD2 as anti-colon cancer agents. Bioorg Chem. 2026;175:109822. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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