| S8276 |
FCCP
|
FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes. |
-
Nature, 2025, 10.1038/s41586-024-08395-9
-
Nat Commun, 2025, 16(1):3012
-
Cell Death Dis, 2025, 16(1):163
|
|
| S8731 |
IACS-010759 (IACS-10759)
|
IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I. |
-
Cell Rep, 2025, 44(7):115901
-
Cell Commun Signal, 2025, 23(1):47
-
Sci Adv, 2025, 11(28):eadu5915
|
|
| S8828 |
Gboxin
|
Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes. |
-
Cell Rep, 2025, 44(7):115901
-
Cell Rep, 2024, 43(10):114775
-
Mol Oncol, 2023, 17(9):1821-1843
|
|
| S8943 |
VLX600
|
VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. |
-
Cancers (Basel), 2022, 14(13)3225
|
|
| S0096 |
S-Gboxin
|
S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM. |
-
STAR Protoc, 2025, 6(2):103719
-
Cell Rep Med, 2024, 5(10):101757
-
EMBO Mol Med, 2022, 14(12):e16082
|
|
| F2814New |
NDUFS2 Antibody [N8J1]
|
|
|
|
| S2987 |
4-Methyl-2-oxovaleric acid
|
4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity. |
-
Nature, 2024, 10.1038/s41586-024-08307-x
|
|
| E4709 |
MS-L6
|
MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy. |
|
|
| S9736New |
ME-344
|
ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM. |
|
|
| E5927New |
Mito-LND (Mito-Lonidamine)
|
ミト-LND(ミト-ロニダミン)は、経口活性を持ち、ミトコンドリアを標的とする酸化的リン酸化(OXPHOS)の阻害剤です。ミト-LNDは、ミトコンドリアのエネルギー代謝を阻害し、活性酸素種の生成を促進し、肺癌細胞においてオートファジー性細胞死を誘導します。 |
|
|
| E1139 |
DX3-213B
|
DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor with IC50 of 3.6 nM, and impairs ATP generation with IC50 of 11 nM. |
|
|
| S9604 |
Lixumistat (IM156)
|
Lixumistat (IM156), is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors. |
-
bioRxiv, 2024, 2024.09.16.613317
|
|
| E1149 |
BAY-179
|
BAY-179 is an excellent in vivo suitable tool with which to probe the biological relevance of complex I inhibition in cancer indications. |
|
|
| S5604 |
Diphenylamine Hydrochloride
|
Diphenylamine (N-Phenylbenzenamine, Anilinobenzene, C.I. 10355), a derivative of aniline, is widely used as an industrial antioxidant, dye mordant and reagent and is also employed in agriculture as a fungicide and antihelmintic. |
|
|
| S8276 |
FCCP
|
FCCP (Trifluoromethoxy carbonylcyanide phenylhydrazone, Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone) is a potent uncoupler of oxidative phosphorylation in mitochondria that disrupts ATP synthesis by transporting protons across cell membranes. |
- Nature, 2025, 10.1038/s41586-024-08395-9
- Nat Commun, 2025, 16(1):3012
- Cell Death Dis, 2025, 16(1):163
|
|
| S8731 |
IACS-010759 (IACS-10759)
|
IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I. |
- Cell Rep, 2025, 44(7):115901
- Cell Commun Signal, 2025, 23(1):47
- Sci Adv, 2025, 11(28):eadu5915
|
|
| S8828 |
Gboxin
|
Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes. |
- Cell Rep, 2025, 44(7):115901
- Cell Rep, 2024, 43(10):114775
- Mol Oncol, 2023, 17(9):1821-1843
|
|
| S8943 |
VLX600
|
VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS), potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. |
- Cancers (Basel), 2022, 14(13)3225
|
|
| S0096 |
S-Gboxin
|
S-Gboxin, a functional analogue of Gboxin, is an oxidative phosphorylation (OXPHOS) inhibitor which inhibits growth of mouse and human glioblastoma (GBM) with IC50 of 470 nM. |
- STAR Protoc, 2025, 6(2):103719
- Cell Rep Med, 2024, 5(10):101757
- EMBO Mol Med, 2022, 14(12):e16082
|
|
| S2987 |
4-Methyl-2-oxovaleric acid
|
4-Methyl-2-oxovaleric acid (Ketoleucine, 4-MOV, KIC, 4-Methyl-2-oxopentanoic acid, alpha-Ketoisocaproic acid, alpha-ketoisocaproate, 2-Oxoisohexanoate) is released by Astrocytes to neurons and can be reaminated by aminotransferase to leucine. 4-Methyl-2-oxovaleric acid reduces the rate of protein degradation in skeletal muscle. 4-Methyl-2-oxovaleric acid acts as an uncoupler of oxidative phosphorylation (OXPHOS) and as a metabolic inhibitor possibly through its inhibitory effect on alpha-ketoglutarate dehydrogenase (oxoglutarate dehydrogenase complex, OGDC) activity. |
- Nature, 2024, 10.1038/s41586-024-08307-x
|
|
| E4709 |
MS-L6
|
MS-L6(Agn-PC-0N3ahi, NSC34338) is a potent inhibitor of OXPHOS, targeting electron transport chain complexes I (ETC-I), combining inhibition of NADH oxidation and uncoupling effect, on the respiratory chain. It exhibits potent antitumor efficacy. |
|
|
| S9736New |
ME-344
|
ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM. |
|
|
| E5927New |
Mito-LND (Mito-Lonidamine)
|
ミト-LND(ミト-ロニダミン)は、経口活性を持ち、ミトコンドリアを標的とする酸化的リン酸化(OXPHOS)の阻害剤です。ミト-LNDは、ミトコンドリアのエネルギー代謝を阻害し、活性酸素種の生成を促進し、肺癌細胞においてオートファジー性細胞死を誘導します。 |
|
|
| E1139 |
DX3-213B
|
DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor with IC50 of 3.6 nM, and impairs ATP generation with IC50 of 11 nM. |
|
|
| S9604 |
Lixumistat (IM156)
|
Lixumistat (IM156), is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors. |
- bioRxiv, 2024, 2024.09.16.613317
|
|
| E1149 |
BAY-179
|
BAY-179 is an excellent in vivo suitable tool with which to probe the biological relevance of complex I inhibition in cancer indications. |
|
|
| S5604 |
Diphenylamine Hydrochloride
|
Diphenylamine (N-Phenylbenzenamine, Anilinobenzene, C.I. 10355), a derivative of aniline, is widely used as an industrial antioxidant, dye mordant and reagent and is also employed in agriculture as a fungicide and antihelmintic. |
|
|