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Cat. No.: HY-184173

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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.

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

Formula: C₄₉H₅₅BrClF₃N₃O₅PS
Molecular Weight:1001.37

Storage:

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

OXPHOS-IN-3 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

SIRT3

GPX4

All Sirtuin Isoforms :

All Glutathione Peroxidase Isoforms :

GPX1
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.

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, showing IC₅₀ values of 0.27 μM, 6.25 μM, and 3.15 μM against MIAPaCa-2 , PANC-1 , and BxPC-3 cells under hypoxic conditions, respectively.
Exhibited IC₅₀ values of 3.36 μM, 2.07 μM, and 2.06 μM against MIAPaCa-2 , PANC-1 , and BxPC-3 cells under normoxic conditions, respectively.
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.

Chemical Information

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-]
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

Handling Instructions (2659 KB)

References

[1]. Yan H, et al. Dual Metabolic Blockade in Pancreatic Cancer: Potent Anticancer Activity of Mitochondria-Targeted Glycolysis and OXPHOS Inhibitors. J Med Chem. 2026 Jun 11;69(11):13452-13472. [Content Brief]

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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OXPHOS-IN-3

All Sirtuin Isoforms

All Glutathione Peroxidase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

OXPHOS-IN-3 Related Classifications

HY-184173 Related Classifications