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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₄₉H₅₅BrClF₃N₃O₅PS
分子量:1001.37

保管条件:

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

OXPHOS-IN-3 構造式

容量

価格（税別）

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数量

Amount: USD 0.00

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Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

SIRT3

GPX4

Sirtuin アイソフォーム固有の製品をすべて表示 :

Glutathione Peroxidase アイソフォーム固有の製品をすべて表示 :

GPX1
GPX4

体外実験

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.

体内実験

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.

化学情報

分子量 1001.37
分子式 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-]
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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OXPHOS-IN-3

Sirtuin アイソフォーム固有の製品をすべて表示

Glutathione Peroxidase アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

OXPHOS-IN-3 関連分類

HY-184173 関連分類