S7309 |
BAY 87-2243
|
BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1. |
-
Cancers (Basel), 2024, 16(5)976
-
PLoS One, 2024, 19(2):e0299145
-
Mol Ther Nucleic Acids, 2023, 31:421-436
|
|
S7009 |
LCL161
|
LCL-161, a small molecule second mitochondrial activator of caspase (SMAC) mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). |
-
Cell Death Dis, 2024, 15(8):592
-
Cell Death Dis, 2024, 15(4):255
-
PLoS One, 2024, 19(2):e0299577
|
|
S3654 |
Tauroursodeoxycholic Acid (TUDCA)
|
Tauroursodeoxycholic acid (TUDCA) is the taurine conjugate of ursodeoxycholic acid (UDCA) and acts as a mitochondrial stabilizer and anti-apoptotic agent in several models of neurodegenerative diseases, including AD, Parkinson's diseases (PD), and Huntington's diseases (HD). |
-
Cell Mol Life Sci, 2024, 81(1):299
-
iScience, 2023, 26(8):107312
-
Int J Mol Sci, 2023, 24(11)9640
|
|
S9803 |
Elamipretide (MTP-131, SS-31)
|
Elamipretide (MTP-131, SS-31) is a cytochrome c peroxidase inhibitor. Elamipretide improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice. |
-
Emerg Microbes Infect, 2024, 13(1):2382235
-
BMC Biol, 2024, 22(1):33
-
bioRxiv, 2024, 2024.02.22.581432
|
|
S3375 |
Mitochondrial Fusion Promoter M1
|
Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator that increases the expression of mitofusin 2, a mitochondrial outer membrane fusion protein, reduces brain mitochondrial dysfunction. Mitochondrial fusion promoter M1 alleviates brain damage in rats with cardiac ischemia/reperfusion injury. |
-
J Lipid Res, 2024, 65(10):100639
-
Free Radic Biol Med, 2023, 195:270-282
-
Stem Cell Res Ther, 2022, 13(1):127
|
|
S2968 |
CTPI-2
|
CTPI-2 is an inhibitor of mitochondrial citrate carrier SLC25A1 with KD of 3.5 μM. CTPI-2 is a unique regulator of glycolysis that limits the metabolic plasticity of cancer stem cells (CSCs). |
-
J Immunol, 2022, 208(5):1085-1098
-
J Immunol, 2022, 208(5):1085-1098
|
|
S5874 |
D-Carnitine hydrochloride
|
D-Carnitine hydrochloride ((S)-Carnitine hydrochloride, (+)-Carnitine hydrochloride) is biosynthesized from lysine. It might be associated with the energy production from branched chain amino acids. |
-
Med Sci Monit, 2020, 26;26:e923251
|
|
S3296 |
Hispidulin
|
Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. |
-
Evid Based Complement Alternat Med, 2023, 2023:9428241
|
|
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
|
|
S0411 |
BAM 15
|
BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue. |
-
Neuroscience, 2012, 223:238-45
|
|
S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0767 |
NL-1
|
The mitochondrial mitoNEET ligand NL-1 is a mitoNEET inhibitor, which induces a concentration-dependent decrease in cell viability with an IC50 of 47.35 μM and 56.26 μM in REH and REH/Ara-C cells respectively. The docking studies using liver mitochondrial suspensions show the IC50 of NL-1 binding for [3H]-rosiglitazone is 0.9 μM and the Ki for NL-1 site 1 and site 2 was 4.78 and 2.77, respectively. |
-
J Transl Med, 2024, 22(1):593
|
|
E1823New |
Ninerafaxstat trihydrochloride
|
Ninerafaxstat trihydrochloride (MB-1018972 trihydrochloride, IMB-101 trihydrochloride) acts as a competitive inhibitor of 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation. It is an orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride regulates myocardial substrate utilization and improves cardiac efficiency. Ninerafaxstat trihydrochloride is also used in research of cardiovascular diseases. |
|
|
S6268 |
4-Pentenoic acid
|
4-Pentenoic acid (Allylacetic acid, 3-vinylpropionic acid, 4-penten-1-oic acid), a flavouring ingredient, is used to inhibit fatty acid oxidation in rat heart mitochondria. |
|
|
S6036 |
ER-000444793
|
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening with IC50 of 2.8 μM. |
|
|
S2592 |
Emapunil (AC 5216)
|
Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173) is a novel mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) ligand. Emapunil(AC-5216) showes high affinity for MBRs prepared from rat whole brain with Ki of 0.297 nM and IC50 of 3.04 nM and 2.73 nM at rat glioma cells and human glioma cells, respectively. |
|
|
E0032 |
Olesoxime (TRO 19622)
|
Olesoxime (TRO19622) is a novel, orally active and CNS-penetrant mitochondrial-targeted neuroprotective compound.
|
|
|
S2348 |
Rotenone
|
Rotenone is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production. |
-
Cell Rep Med, 2024, 5(5):101519
-
Redox Biol, 2024, 70:103039
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
|
|
S3593 |
Rhodamine 6G
|
Rhodamine 6G (R6G, Basic Red 1, Rhodamine 590) is a fluorescence tracer that binds to mitochondria, thus reducing the intact mitochondria number and inhibiting mitochondrial metabolic activity. |
|
|
S0012 |
E260
|
E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. |
|
|
E1252 |
MitoPQ
|
MitoPQ (MitoParaquat), a mitochondria-targeted redox cycler, enables the selective generation of superoxide within mitochondria and is a useful tool to investigate the many roles of mitochondrial superoxide in pathology and redox signaling in cells and in vivo. |
|
|
S7309 |
BAY 87-2243
|
BAY 87-2243 is a potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor. BAY 87-2243 inhibits mitochondrial complex I activity, thus triggering a mitophagy-dependent ROS increase leading to necroptosis and ferroptosis. BAY 87-2243 exerts antitumor activity. Phase 1. |
- Cancers (Basel), 2024, 16(5)976
- PLoS One, 2024, 19(2):e0299145
- Mol Ther Nucleic Acids, 2023, 31:421-436
|
|
S2968 |
CTPI-2
|
CTPI-2 is an inhibitor of mitochondrial citrate carrier SLC25A1 with KD of 3.5 μM. CTPI-2 is a unique regulator of glycolysis that limits the metabolic plasticity of cancer stem cells (CSCs). |
- J Immunol, 2022, 208(5):1085-1098
- J Immunol, 2022, 208(5):1085-1098
|
|
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
|
|
S3264 |
Atractyloside potassium salt
|
Atractyloside potassium salt (ATR potassium salt), a toxic diterpenoid glycoside isolated from the fruits of Xanthium sibiricum (Cang'erzi), is a powerful and specific inhibitor of mitochondrial ADP/ATP carriers. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. |
|
|
S0767 |
NL-1
|
The mitochondrial mitoNEET ligand NL-1 is a mitoNEET inhibitor, which induces a concentration-dependent decrease in cell viability with an IC50 of 47.35 μM and 56.26 μM in REH and REH/Ara-C cells respectively. The docking studies using liver mitochondrial suspensions show the IC50 of NL-1 binding for [3H]-rosiglitazone is 0.9 μM and the Ki for NL-1 site 1 and site 2 was 4.78 and 2.77, respectively. |
- J Transl Med, 2024, 22(1):593
|
|
E1823New |
Ninerafaxstat trihydrochloride
|
Ninerafaxstat trihydrochloride (MB-1018972 trihydrochloride, IMB-101 trihydrochloride) acts as a competitive inhibitor of 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation. It is an orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride regulates myocardial substrate utilization and improves cardiac efficiency. Ninerafaxstat trihydrochloride is also used in research of cardiovascular diseases. |
|
|
S6268 |
4-Pentenoic acid
|
4-Pentenoic acid (Allylacetic acid, 3-vinylpropionic acid, 4-penten-1-oic acid), a flavouring ingredient, is used to inhibit fatty acid oxidation in rat heart mitochondria. |
|
|
S6036 |
ER-000444793
|
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening with IC50 of 2.8 μM. |
|
|
S3593 |
Rhodamine 6G
|
Rhodamine 6G (R6G, Basic Red 1, Rhodamine 590) is a fluorescence tracer that binds to mitochondria, thus reducing the intact mitochondria number and inhibiting mitochondrial metabolic activity. |
|
|
S9803 |
Elamipretide (MTP-131, SS-31)
|
Elamipretide (MTP-131, SS-31) is a cytochrome c peroxidase inhibitor. Elamipretide improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice. |
- Emerg Microbes Infect, 2024, 13(1):2382235
- BMC Biol, 2024, 22(1):33
- bioRxiv, 2024, 2024.02.22.581432
|
|
S3375 |
Mitochondrial Fusion Promoter M1
|
Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator that increases the expression of mitofusin 2, a mitochondrial outer membrane fusion protein, reduces brain mitochondrial dysfunction. Mitochondrial fusion promoter M1 alleviates brain damage in rats with cardiac ischemia/reperfusion injury. |
- J Lipid Res, 2024, 65(10):100639
- Free Radic Biol Med, 2023, 195:270-282
- Stem Cell Res Ther, 2022, 13(1):127
|
|
S3296 |
Hispidulin
|
Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. |
- Evid Based Complement Alternat Med, 2023, 2023:9428241
|
|
S0411 |
BAM 15
|
BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue. |
- Neuroscience, 2012, 223:238-45
|
|
S2592 |
Emapunil (AC 5216)
|
Emapunil (AC-5216, 18 kiloDalton Translocator Protein, XBD173) is a novel mitochondrial benzodiazepine receptor/translocator protein (MBR/TSPO) ligand. Emapunil(AC-5216) showes high affinity for MBRs prepared from rat whole brain with Ki of 0.297 nM and IC50 of 3.04 nM and 2.73 nM at rat glioma cells and human glioma cells, respectively. |
|
|
S2348 |
Rotenone
|
Rotenone is a botanical insecticide that is an inhibitor of mitochondrial electron transport. Rotenone inhibits NADH/DB oxidoreductase and NADH oxidase with IC50 of 28.8 nM and 5.1 nM, respectively. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production. |
- Cell Rep Med, 2024, 5(5):101519
- Redox Biol, 2024, 70:103039
- Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
|
|
S0012 |
E260
|
E260 (Fer and FerT inhibitor E260) is a Fer kinase and FerT inhibitor that selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. |
|
|