OXPHOS-IN-2 

OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC₅₀ = 12.3 nM) and Bxpc-3 cells (IC₅₀ = 250 nM in glucose medium, IC₅₀ = 17.5 nM in galactose medium). OXPHOS-IN-2 regulates the NADH/NAD⁺ ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer^[1].

OXPHOS-IN-2 (Compound 28c) (0-1000 μM，12 小时) 降低 PC9 细胞中 ATP 和 NAD₊/NADH 的比率，并抑制 AMPK 磷酸化^[1]。
OXPHOS-IN-2 (0-20 nM，14 天) 显著抑制 PC9 细胞的集落形成能力^[1]。
OXPHOS-IN-2 (0-1 μM) 可以通过剂量依赖性地增加 PC9 和 Bxpc-3 细胞中的活性氧 ROS 水平并降低线粒体膜电位诱导细胞凋亡^[1]。
OXPHOS-IN-2 (0-50 nM) 诱导 PC9 细胞 DNA 损伤并增加 γ-H2AX 的表达^[1]。
OXPHOS-IN-2 可以抑制多种肿瘤细胞系在葡萄糖和半乳糖培养基中的增殖，包括H1975 (IC₅₀ = 6.43 nM 和 29.5 nM)，H2228 (IC₅₀ = 4.54 nM和 21.5 nM)，KP-4 (IC₅₀ = 3.61 nM 和 48.7 nM)，MKN45 (IC₅₀ = 5.78 nM 和 29.8 nM)，HCT116 (IC₅₀ = 5.19 nM 和 31.2 nM)，MDA-MB-231 (IC₅₀ = 1.31 nM 和 7.5 nM)，MHCC-97H (IC₅₀ = 1.76 nM 和 12.4 nM) 和 SiHA (IC₅₀ = 5.10 nM 和 35.1 nM) 细胞^[1]。

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

OXPHOS-IN-2 (Compound 28c) (7.5 mg/kg；口服；每天一次；持续 14 天) 在雄性 BALB/c-nu PC9 肿瘤小鼠中显著抑制肿瘤生长且具有良好的安全性^[1]。

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

588.60

C₂₇H₂₇F₃N₆O₄S

Room temperature in continental US; may vary elsewhere.

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

• [1]. Cao L, et al. Synthesis and evaluation of new 5-(1H-1,2,4-triazol-3-yl)-1,2,4-oxadiazole derivatives and their application as OXPHOS inhibitors. Eur J Med Chem. 2025 Jun 25;297:117903.  [Content Brief]