oxphos

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].

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.

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

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.

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.

BAM 15 is an uncoupler of mitochondrial protonophore.

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).

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.

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

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

TRAP1-IN-1 (compound 35) is a potent, selective TRAP1 inhibitor affecting the mitochondrial variant of Hsp90. It exhibits over 250-fold greater selectivity for TRAP1 compared to Grp94, destabilizes TRAP1 tetramers, and promotes the degradation of TRAP1 client proteins. Additionally, TRAP1-IN-1 impedes mitochondrial complex I activity involved in oxidative phosphorylation (OXPHOS), compromises the mitochondrial membrane potential, and augments glycolytic metabolism [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].

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 .

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.

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].

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].

Grossamide (GSE) Grossamide is a lignan amide derived from thioguanosine.6-Thioguanosine (GSE) is a selective and potent miR-210 (miRNA-210) inhibitor.6-Thioguanosine (GSE) is a selective and potent miR-210 (miRNA-210) inhibitor.6-Thioguanosine (GSE) is a selective and potent miR-210 (miRNA-210) inhibitor that inhibits pre-miR-210 processing and induces apoptosis in breast cancer cells.

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

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].

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].

IACS-010759 is a potent inhibitor of complex I of OXPHOS with orally bioavailable. IACS-10759 effectively inhibits ATP production and oxygen consumption in isolated mitochondria, and inhibits the conversion of NADH to NAD+ in immunoprecipitated complex I

DX3-235 is an inhibitor of oxidative phosphorylation (OXPHOS). In galactose-containing media, DX3-235 inhibits complex I function and ATP production by nanomolar amounts and is significantly cytotoxic.

DX3-234 is an inhibitor of oxidative phosphorylation (OXPHOS). In a Pan02 homozygous model of pancreatic cancer, DX3-234 exhibits significant tumour suppressive activity.

NMac1is a small molecule phenylbutenoid dimer that has novel anti-proliferative effect only under glucose starvation in metastatic breast cancer cells. NMac1 causes significant activation of AMPK by decreasing ATP synthesis, lowers mitochondrial membrane potential (MMP, ΔΨm), and inhibits oxygen consumption rate (OCR) under glucose starvation. These effects of NMac1 are provoked by a consequence of OXPHOS complex I inhibition.