D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC).

BJH-60 is a mitochondrial complex 1 inhibitor. BJH-60 can inhibit mitochondrial oxygen consumption rate with an IC50 of 1.9 μM in A549 cells. BJH-60 shows no PDE inhibitory effect. BJH-60 can be used for the research of cancer, such as breast cancer.

PENAO TFA is the trifluoroacetic acid of PENAO. PENAO is a potent tumour cell mitochondrial toxin. PENAO inactivates tumor cell mitochondria by targeting inner-membrane adenine nucleotide transferase.

NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease.

BJH-86 is a soluble mitochondrial complex 1 inhibitor (oxygen consumption rate inhibition IC50 = 5 μM). BJH-86 exhibits weak inhibitory activity against phosphodiesterase 10A (PDE10A) (IC50 >10 μM). BJH-86 can reduce cellular oxygen consumption and inhibit cancer cell proliferation. BJH-86 can be used for the research of cancer, such as lung cancer.

(E/Z)-MitoTam (iodide, hydriodide) (MitoTam (iodide, hydriodide)) is the E/Z mixture of MitoTam iodide, hydriodide. MitoTam iodide, hydriodide is a Tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.

KIT-13 is an orally active plasmalogen derivative to inhibit neuroinflammation and mitochondrial DNA leakage associated with Mecp2 deficiency. KIT-13 significantly reduce neurological symptoms and improves the life span of the Rett Syndrome (RTT) model mice. KIT-13 can be used for the study of RTT and other neuroinflammation-related diseases.

Isoapoptolidin is a mitochondrial F0F1-ATPase inhibitor (Ki>100 μM, selective for mitochondrial complex V). Isoapoptolidin is promising for research of mitochondrial energy metabolism-related diseases (e.g., cancer, neurodegeneration).

ZGL-18 is an uncoupling protein 1 (UCP1)-inspired mitochondrial uncoupler. ZGL-18 activates brown adipocytes and reduces mitochondrial membrane potential.

SHO1122147 (Compound 7m) affects the mitochondrial electron transport chain, exhibits mitochondrial uncoupling activity (EC50=3.6 μM), and increases the oxygen consumption rate (OCR=69%) and promotes cellular respiration. SHO1122147 is orally active, and can be used in reaearch of obesity and metabolic dysfunction-associated steatohepatitis (MASH).

S-15176 is an inhibitor of the mitochondrial permeability transition pore (PTP). S-15176 inhibits mitochondrial swelling induced by tert-butylhydroperoxide with an IC50 value of 45.7 μM. S-15176 inhibits PTP opening, prevents mitochondrial membrane potential dissipation and NAD(P)H oxidation, and increases mitochondrial calcium loading capacity. S-15176 is promising for research of ischemia-reperfusion injury.

PENAO is a potent tumour cell mitochondrial toxin. PENAO inactivates tumor cell mitochondria by targeting inner-membrane adenine nucleotide transferase.

LH1513 is a dioxalate derivative of l-lysine that inhibits CaOx crystallization with better activity than citrate and pyruvate. LH1513 has potential preventive activity in hyperoxaluria models and effectively prevents urinary CaOx crystal formation in Agxt knockout mice. AGXT-1 is a mitochondrial protein involved in metabolism.

BE2647 is a selective inhibitor for mitochondrial pyruvate carrier (MPC) with an EC50 of 70 nM. BE2647 exhibits good metabolic stability in mouse liver microsomes. BE2647 can be used in research of metabolic diseases, non-alcoholic fatty liver disease (MASLD), or non-alcoholic steatohepatitis (MASH).

Bac-429 (compound 23) is a N-acyl amino acid analog that stimulates mitochondrial respiration.

AK-4 is a glucose-lowering agent, acting function as a mitochondrial uncoupler.

THP104c is a mitochondrial fission inhibitor.

Clidanac is a potent anti-inflammatory agent. Clidanac can uncouple the oxidative phosphorylation and can be used for the research of rheumatoid arthritis.

D-Histidine is an enantiomer of L-histidine. L-Histidine is an essential amino acid for infants. L-Histidine is an inhibitor of mitochondrial glutamine transport.

MFI8 is a small molecule inhibitor of mitochondrial fusion.

BAY-179 is a potent, selective, and species cross-reactive complex I inhibitor (IC50=79 µM).

Complex III-IN-2 (Compd 4d-2) is a complex III inhibitor. Complex III-IN-2 shows antifungal activity with an EC50 of 29.98 mg/L and 29.31 mg/L against sclerotinia sclerotiorum and R. solani, respectively.

Complex III-IN-1 (Compd 4c-2) is a complex III inhibitor. Complex III-IN-1 shows antifungal activity with an EC50 of 18.53 mg/L against sclerotinia sclerotiorum.

DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer.

DX2-201 is a potent and selective oxidative phosphorylation (OXPHOS) complex I inhibitor with an IC50 of 312 nM. DX2-201 has anticancer effects.

RYL-552, a mitochondrial electron transport chain (ETC) inhibitor, is a P. falciparum NADH dehydrogenase 2 (PfNDH2) inhibtor.

NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway.

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor. DX3-235 shows nanomolar inhibition of complex I function and ATP production in a galactose-containing medium resulting in significant cytotoxicity.

DX3-234 is an oxidative phosphorylation (OXPHOS) inhibitor. DX3-234 shows significant tumor suppression in the Pan02 syngeneic model of pancreatic cancer.

Menadiol (Dihydrovitamin K3), a menaquinol analogue, is an electron donor for reversed oxidative phosphorylation in submitochondrial particles.