2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Oxidative Phosphorylation PDK-1 Ferroptosis Mitochondrial Metabolism Sirtuin Glutathione Peroxidase
  4. OXPHOS-IN-3

OXPHOS-IN-3 is a mitochondria-targeted dual OXPHOS/glycolysis inhibitor. OXPHOS-IN-3 exhibits potent antiproliferative activity against pancreatic cancer cells. OXPHOS-IN-3 induces mitochondrial dysfunction, ferroptosis, and immunogenic cell death (ICD). OXPHOS-IN-3 shows potent antitumor activity in pancreatic ductal adenocarcinoma (PDAC) models.

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OXPHOS-IN-3

OXPHOS-IN-3 Chemical Structure

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OXPHOS-IN-3 Related Antibodies

Top Publications Citing Use of Products

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Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7 SIRT4

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GPX1 GPX4

  • Biological Activity

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  • References

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Description

OXPHOS-IN-3 is a mitochondria-targeted dual OXPHOS/glycolysis inhibitor. OXPHOS-IN-3 exhibits potent antiproliferative activity against pancreatic cancer cells. OXPHOS-IN-3 induces mitochondrial dysfunction, ferroptosis, and immunogenic cell death (ICD). OXPHOS-IN-3 shows potent antitumor activity in pancreatic ductal adenocarcinoma (PDAC) models[1].

IC50 & Target

SIRT3

 

GPX4

 

In Vitro

OXPHOS-IN-3 (Compound 14c) (0.1-0.8 μM; 24-72 h) exhibits potent antiproliferative activity in hypoxic MIAPaCa-2 cells (IC50 = 0.27 μM) with good selectivity over normal HS-5 and L02 cells (IC50 > 20 μM)[1].
OXPHOS-IN-3 (0.1-0.8 μM; 24-72 h) dose-dependently inhibits colony formation, migration, and invasion while downregulating epithelial-mesenchymal transition (EMT) markers in hypoxic MIAPaCa-2 cells[1].
OXPHOS-IN-3 (0.1-2.0 μM; 12-72 h) inhibits PDKs (IC50 = 97.8 nM), reduces PDH phosphorylation (EC50 = 14.3 nM), decreases lactate production, and suppresses glycolytic parameters under hypoxic conditions[1].
OXPHOS-IN-3 (0.2-2.0 μM; 12-48 h) downregulates SDHB and SIRT3, induces mitochondrial dysfunction and triggers ferroptosis with low apoptosis level in hypoxic MIAPaCa-2 cells[1].
OXPHOS-IN-3 (0.2-2.0 μM; 12-48 h) induces mitochondrial ROS accumulation, MMP collapse, mPTP opening, and cytochrome c release in MIAPaCa-2 cells[1].
OXPHOS-IN-3 (0.2-2.0 μM; 12-24 h) induces immunogenic cell death hallmarks in human MIAPaCa-2 cells, including CRT surface exposure, HMGB1 translocation/release, and intracellular ATP depletion[1].

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

OXPHOS-IN-3 Related Antibodies

Cell Viability Assay[1]

Cell Line: MIAPaCa-2, PANC-1, BxPC-3 (normoxic and hypoxic), HS-5, L02 cells
Concentration: 0.1, 0.4, 0.8 μM (and broader range for IC50 determination)
Incubation Time: 24-72 h
Result: Inhibited cell viability in PDAC cells under hypoxic conditions with an IC50 of 0.27 μM in MIAPaCa-2 cells.
Showed markedly reduced cytotoxicity to normal HS-5 and L02 cells (IC50 > 20 μM).

Cell Proliferation Assay[1]

Cell Line: MIAPaCa-2 cells (hypoxic)
Concentration: 0.1, 0.4, 0.8 μM
Incubation Time: 72 h (followed by 10-14 days culture)
Result: Dose-dependently suppressed clonogenic capacity, while Gemcitabine (HY-17026) showed weakened effect under hypoxia.

Cell Migration Assay [1]

Cell Line: MIAPaCa-2 cells (hypoxic)
Concentration: 0.1, 0.4, 0.8 μM
Incubation Time: 24 h
Result: Significantly inhibited wound healing and transwell migration.

Cell Invasion Assay[1]

Cell Line: MIAPaCa-2 cells (hypoxic, Matrigel-coated)
Concentration: 0.1, 0.4, 0.8 μM
Incubation Time: 48 h
Result: Effectively inhibited the invasive potential of MIAPaCa-2 cells under hypoxic conditions

Western Blot Analysis[1]

Cell Line: MIAPaCa-2 (hypoxic), PANC-1, BxPC-3 cells
Concentration: 0.2, 1.0, 2.0 μM
Incubation Time: 12-72 h
Result: Reduced expression of p-PDH, SDHB, SIRT3, EMT markers (ZEB1, Slug, Vimentin, Snail, N-cadherin), xCT and GPX4.
Increased HIF-1α and PDK1 expression under hypoxic validation.

Immunofluorescence[1]

Cell Line: MIAPaCa-2 cells (hypoxic)
Concentration: 0.2, 1.0, 2.0 μM
Incubation Time: 12-24 h
Result: Promoted CRT surface exposure and HMGB1 nuclear-to-cytoplasmic translocation, visualized by confocal microscopy.

Apoptosis Analysis[1]

Cell Line: MIAPaCa-2 cells (hypoxic)
Concentration: 0.2, 1.0, 2.0 μM
Incubation Time: 24-48 h
Result: Induced only low-level apoptosis (≤15%), which was not the primary mode of cell death.
In Vivo

OXPHOS-IN-3 (Compound 14c) (5 mg/kg; i.t.; every 2 days for 3 doses) significantly suppresses both primary tumor growth and distal untreated tumor growth in the syngeneic bilateral PANC02 model in C57BL/6 mice, demonstrating systemic antitumor immunity[1].
OXPHOS-IN-3 (5 and 10 mg/kg; i.p.; every 2 days for 6 doses) dose-dependently inhibits tumor growth in the syngeneic PANC02-EGFP subcutaneous model in C57BL/6 mice, accompanied by downregulation of p-PDH, SDHB, SIRT3, and EMT markers in tumor tissues[1].

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

Animal Model: Syngeneic bilateral PANC02 model (Male C57BL/6 mice, 6-8 weeks old)[1]
Dosage: 5 mg/kg
Administration: Intratumoral injection (i.t.), every 2 days for 3 doses
Result: Reduced primary and contralateral tumor volume/weight compared with control and Gemcitabine (HY-17026) groups.
Decreased Arg-1 and MRC-1 expression in tumor tissues (M1-like TAM reprogramming).
Enhanced HMGB1 release and CRT exposure in tumor sections (IHC/IF).
No significant body weight loss.
Animal Model: Syngeneic PANC02-EGFP subcutaneous model (Male C57BL/6 mice, 6-8 weeks old)[1]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), every 2 days for 6 doses
Result: Dose-dependently inhibited tumor growth as shown by reduced EGFP fluorescence, caliper measurement, and tumor weight.
Decreased p-PDH, SDHB, SIRT3, and EMT markers in tumor tissues.
Showed pronounced tumor cell damage with normal histology in major organs (heart, liver, spleen, lung, kidney).
Exhibited good tolerability with stable body weight throughout the treatment period.
Molecular Weight

1001.37

Formula

C49H55BrClF3N3O5PS
SMILES

ClC1=C(C=CC(S(C2=CC=C(C=C2)C(N3CCN(CC3)CCCCCCCCCC[P+](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)=O)(=O)=O)=C1)NC([C@@](C(F)(F)F)(C)O)=O.[Br-]
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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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OXPHOS-IN-3 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:

OXPHOS-IN-3Oxidative PhosphorylationPDK-1FerroptosisMitochondrial MetabolismSirtuinGlutathione Peroxidase3-Phosphoinositide-dependent protein kinase 1OXPHOSGlycolysisCancer MetabolismMetabolic ReprogrammingMitochondriaMitochondrial DysfunctionImmunogenic Cell DeathPancreatic CancerPancreatic Ductal AdenocarcinomaPDACOrthotopic Pancreatic Cancer ModelSyngeneic Tumor ModelTumor Immune MicroenvironmentROSInhibitorinhibitorinhibit

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