oxidative phosphorylation (oxphos)

Acetyl Coenzyme A trisodium (Acetyl-CoA trisodium) is an important compound in glucose metabolism and lipid metabolism and is involved in the tricarboxylic acid cycle.

VLX600 is an iron-chelating oxidative phosphorylation (OXPHOS) inhibitor, is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

IM156 (HL156A; HL271 acetate) is a chemical derivative of Metformin. IM156 is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model [1] [2]. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which is able to be used for the research of solid tumors [3].

Mito-LND (Mito-Loidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation.

IMT1B (LDC203974) is an orally administered, specific noncompetitive allosteric inhibitor of mitochondrial RNA polymerase (POLRMT), effectively suppressing mitochondrial DNA (mtDNA) expression and conferring anti-tumor properties.

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

DX3-234 is a potent oxidative phosphorylation (OXPHOS) inhibitor that acts by inhibiting complex I in the mitochondrial electron transport chain (ETC), leading to intracellular ATP depletion and cell death, and can be used for the treatment of specific cancers dependent on aerobic metabolism, such as pancreatic cancer.

DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor with nanomolar-level inhibitory effects on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP production, leading to impaired cellular energy metabolism and cancer cytotoxicity.

BAM 15 is an uncoupler of mitochondrial protonophore.

JWJ-01-306 is a molecular glue that targets the C2H2 zinc finger transcription factor ZBTB11. It effectively degrades ZBTB11, reduces oxidative phosphorylation (OXPHOS) and the tricarboxylic acid (TCA) cycle, and inhibits the proliferation of KAS-resistant PDAC cells. In mouse models, JWJ-01-306 demonstrates favorable pharmacokinetic properties.

IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats .

IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain.

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

OXPHOS-IN-1 (compound 2) is an inhibitor of oxidative phosphorylation (OXPHOS) that inhibits the growth of MIA PaCa-2 cells (IC50: 2.34 μM) and BxPC-3 cells (IC50: 13.82 μM).

DX3-213B is a potent, orally active inhibitor of oxidative phosphorylation (OXPHOS) complex I with an IC50 of 3.6 nM. DX3-213B blocks ATP production (IC50: 11 nM) and inhibits the growth of MIA PaCa-2 cells (GI50: 11 nM). DX3-213B can be used to study pancreatic cancer.

FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. FCCP is often used as an apoptosis inducer.

Calcimycin (A-23187) hemimagnesium, an antibiotic and divalent cation ionophore (such as calcium and magnesium), serves various biological roles. It triggers Ca2+-dependent cell death by elevating intracellular calcium levels and suppresses the growth of Gram-positive bacteria and certain fungi. Additionally, this compound hinders ATPase activity and uncouples oxidative phosphorylation (OXPHOS) in mammalian cells, ultimately leading to apoptosis [1] [2] [3] [4].

AMPK Activator 11 is a nanomolar potent inhibitor of cell proliferation in various colorectal carcinomas (CRCs), acting through the selective activation of AMP-activated protein kinase (AMPK) and enhancement of oxidative phosphorylation (OXPHOS) (mitochondrial metabolism). This compound demonstrates particular efficacy in inhibiting RKO xenograft growth, rendering it useful for anti-tumor and metabolic disease research [1].

TRAP1-IN-1 (compound 35) is a selective TRAP1 inhibitor that disrupts TRAP1 tetramer stability, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.

TRAP1-IN-2, also known as compound 36, is a selective degrader of the TRAP1 client protein that does not affect Hsp90-cytosolic clients. It inhibits oxidative phosphorylation (OXPHOS) and shifts cellular metabolism toward glycolysis. Additionally, TRAP1-IN-2 compromises the stability of the TRAP1 tetramer and disrupts the mitochondrial membrane potential [1].

SCAL-255 is a mitochondrial complex I (CI) inhibitor, exhibiting potent inhibition with an IC50 of 1.14 μM. It impedes mitochondrial function by blocking oxygen consumption rate (OCR), inducing reactive oxygen species (ROS) production, and diminishing mitochondrial membrane potential (MMP). Furthermore, SCAL-255 significantly hampers the proliferation of cancer cells reliant on oxidative phosphorylation (OXPHOS) [1].

SCAL-266, a potent inhibitor of mitochondrial complex I (CI), exhibits an IC50 of 0.83 μM. This compound impairs mitochondrial function by blocking oxidative phosphorylation (OXPHOS), inhibiting oxygen consumption rate (OCR), increasing reactive oxygen species (ROS) production, and diminishing mitochondrial membrane potential (MMP). Furthermore, SCAL-266 demonstrates significant antiproliferative activity against OXPHOS-dependent cancer cells [1].

ERG245 is a BCAT1 inhibitor that promotes oxidative phosphorylation (OXPHOS) in CD8+ T cells by selectively inhibiting the enzymatic activity of BCAT1, thereby increasing the cytotoxic capacity of CD8+ T cells. ERG245, when administered in combination with the anti-PD-1 antibody Pembrolizumab, induces tumor regression in preclinical settings, and it can be used as a research agent within the field of immuno-oncology.