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 h) reduces the ratio of ATP and NAD₊/NADH and inhibits AMPK phosphorylation in PC9 cells^[1].
OXPHOS-IN-2 (0-20 nM, 14 days) significantly inhibits the colony forming ability of PC9 cells^[1].
OXPHOS-IN-2 (0-1 μM) can induce apoptosis by dose dependently increasing reactive oxygen species (ROS) levels and reducing mitochondrial membrane potential in PC9 and Bxpc-3 cells^[1].
OXPHOS-IN-2 (0-50 nM) induces DNA damage and increases the expression of γ-H2AX in PC9 cells^[1].
OXPHOS-IN-2 can inhibit the proliferation of various tumor cell lines in glucose and galactose medium, including H1975 (IC₅₀ = 6.43 nM and 29.5 nM), H2228 (IC₅₀ = 4.54 nM and 21.5 nM), KP-4 (IC₅₀ = 3.61 nM and 48.7 nM), MKN45 (IC₅₀ = 5.78 nM and 29.8 nM), HCT116 (IC₅₀ = 5.19 nM and 31.2 nM), MDA-MB-231 (IC₅₀ = 1.31 nM and 7.5 nM), MHCC-97H (IC₅₀ = 1.76 nM and 12.4 nM) and SiHA (IC₅₀ = 5.10 nM and 35.1 nM) cells^[1].

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

OXPHOS-IN-2 (Compound 28c) (7.5 mg/kg; p.o.; once daily; for 14 days) significantly inhibits tumor growth and has good safety in PC9 modeled male BALB/c-nu mice^[1].

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

588.60

C₂₇H₂₇F₃N₆O₄S

FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC=CC(N5CCC(S(=O)(C)=O)CC5)=C4)C(C6CC6)=N3)=N2)C=C1

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]