2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD) Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism
  4. 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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MTHFD2-IN-8

MTHFD2-IN-8 Chemical Structure

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MTHFD2-IN-8 Related Antibodies

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Description

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[1].

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.

MTHFD2-IN-8 Related Antibodies

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.
Molecular Weight

723.63

Formula

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-]
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
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MTHFD2-IN-8 Related Classifications

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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:

MTHFD2-IN-8Methylenetetrahydrofolate Dehydrogenase (MTHFD)Reactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismSW620apoptosisHCT116MTHFD2G0/G1 phasereactive oxygen speciescolon cancer cellsCT26mitochondrial membrane potential depolarizationA549Inhibitorinhibitorinhibit

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