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KMG-301AM TFA is the acetoxy methyl esterified form of KMG-301. KMG-301AM TFA successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg 2+-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrialmembrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrialmembrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg 2+ transport across the mitochondrialmembrane in the early phases of a cellular model .
DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrialmembrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
MitoTam bromide, hydrobromide, a Tamoxifen derivative , is an electron transport chain (ETC) inhibitor. MitoTam bromide, hydrobromide reduces mitochondrialmembrane potential in senescent cells and affects mitochondrial morphology . MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells .
MitoTam iodide, hydriodide is a Tamoxifen derivative , an electron transport chain (ETC) inhibitor, spreduces mitochondrialmembrane 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 .
BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons .
BI-10 is an antifungal compound. BI-10 combined with Fluconazole can inhibit hyphal growth, result in ROS accumulation, and decrease mitochondrialmembrane potential (MMP) as well as altering membrane permeability .
6BrCaQ-C10-TPP is a potent mitochondrial heat shock protein TRAP1 inhibitor, with antiproliferative activity in various human cancer cells (IC50=0.008-0.30 μM). 6BrCaQ-C10-TPP can also induces mitochondrialmembrane disturbance .
KMG-301AM is the acetoxy methyl esterified form of KMG-301. KMG-301AM successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg 2+-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrialmembrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrialmembrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg 2+ transport across the mitochondrialmembrane in the early phases of a cellular model .
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrialmembrane potential .
Me4Phen (compound 3) is an oxygen rhenium (V) complex that depletes mitochondrialmembrane potential and upregulates intracellular reactive oxygen species (ROS), leading to endoplasmic reticulum stress-mediated necrosis of cancer cells. Me4Phen is highly lipophilic and effectively overcomes Cisplatin (HY-17394) resistance in a variety of cancer cells .
Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrialmembrane potential and induces DNA damage to induces leukemia cells apoptosis .
MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity .
Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrialmembrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity .
Didocosahexaenoin, an omega-3 derivative, is a diglyceride of DHA and can be synthesised from DHA triglycerides. Didocosahexaenoin causes significant loss of mitochondrialmembrane potential and induces ROS production. Didocosahexaenoin induces apoptosis. Didocosahexaenoin induces stronger cytotoxicity than DHA in human prostate carcinoma cells .
Anticancer agent 39 (compound B12), a fluorescent derivative of Jiyuan Oridonin A (JOA), induces the collapse of mitochondrialmembrane potential (MMP)and thus induced apoptosis.Anticancer agent 39 inhibits cell cloning and migration.Anticancer agent 39 exhibits promising anti-proliferative activity against HGC-27 cells with IC50 value of 0.39 μM .
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrialmembrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrialmembrane depolarization and Bad dephosphorylation .
2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrialmembrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3 .
NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrialmembrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression .
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrialmembrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrialmembrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrialmembrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
TRAP1-IN-2 (compound 36) is a selective degrader of TRAP1 downstream proteins without affecting Hsp90's cytoplasmic downstream proteins. TRAP1-IN-2 also inhibits OXPHOS and alters cellular glycolysis metabolism. TRAP1-IN-2 destabilizes TRAP1 tetramers and disrupts mitochondrialmembrane potential.
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrialmembrane depolarization .
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrialmembrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
HBmito Crimson is a deep red fluorescent probe (λex: 658 nm, λem: 678 nm) for the inner mitochondrialmembrane. HBmito Crimson is a cell membrane-permeable probe with high selectivity for the mitochondrial inner membrane, suitable for specific fluorescence staining of the inner mitochondrialmembrane in living cells. HBmito Crimson has high photostability and brightness, suitable for long-term dynamic fluorescence imaging.
Mito Red is a vital dye and mitochondrial stain that can be used to detect and evaluate mitochondrial function and status. Mito Red accumulates in mitochondria, and its fluorescence intensity is positively correlated with mitochondrialmembrane potential. When the mitochondrialmembrane potential increases, the fluorescence signal of Mito Red increases .
POPSO is a zwitterionic buffer, increases osmolality and shows marked inhibition of anion uniport. POPSO inhibits chloride uniport with an IC50 value of 24 mM. POPSO enhances copper uptake and toxicity in alga, impairs mitochondrial inner membrane. The working pH range of POPSO sesquisodium salt is 7.2-8.5 .
Mito-Tracker Green is a green fluorescent dye that selectively accumulates in the mitochondrial matrix. MitoTracker Green FM covalently binds mitochondrial proteins by reacting with free mercaptan of cysteine residues, allowing staining of mitochondrialmembrane potential independent of membrane potential. Excitation/emission wavelength 490/523 nm.
Pezadeftide is a potent antifungal peptide. Pezadeftide can enter fungal cells and cause a rapid mitochondrial response that results in hyperpolarization of the mitochondrialmembrane .
MitoTracker Deep Red FM fluorescent dye that selectively accumulates in the mitochondrial matrix. MitoTracker Deep Red FM covalently binds mitochondrial proteins by reacting with free mercaptan of cysteine residues, allowing staining of mitochondrialmembrane potential independent of membrane potential. Excitation/emission wavelength 644/665 nm . Storage: Keep away from light.
Mitochondrial respiration-IN-3 is the fluorine derivative of Dalfopristin (HY-A0241). Mitochondrial respiration-IN-3 has cell membrane-permeable. Mitochondrial respiration-IN-3 can inhibit mitochondrial translation of glioblastoma stem cells. Mitochondrial respiration-IN-3 can be used in research of cancer .
TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrialautophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrialmembrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrialmembrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity .
Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses
.
Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans . Bongkrekic acid specific ligand for mitochondrialadenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport .
SL-017 is a novel photoacoustic sensitizer and a derivative of photofrin B. It can be taken up by cells to the maximum extent within 30 minutes and is mainly localized in mitochondria. After being activated by visible light or ultrasound, SL-017 can significantly increase the production of reactive oxygen species (ROS). Low concentrations of SL-017 can rapidly cause the loss of mitochondrialmembrane potential. SL-017 can also cause mitochondrial fragmentation, a process that occurs after the loss of membrane potential. Epoxyeicosatrienoic acids (EETs) can alleviate the loss of mitochondrialmembrane potential caused by SL-017, but the antioxidant ascorbic acid has no such effect. These characteristics indicate that SL-017 mainly targets mitochondria and exerts its cytotoxic effect by triggering the collapse of mitochondrialmembrane potential, generating ROS, and causing mitochondrial fragmentation. As a novel photoacoustic sensitizer, SL-017 has potential application value in photodynamic therapy and sonodynamic therapy.
JC-1 (CBIC2) is an ideal fluorescent probe widely used to detect mitochondrialmembrane potential. JC-1 accumulates in mitochondria in a potential dependent manner and can be used to detect the membrane potential of cells, tissues or purified mitochondria. In normal mitochondria, JC-1 aggregates in the mitochondrial matrix to form a polymer, which emits strong red fluorescence (Ex=488 nm, Em=595 nm); When the mitochondrialmembrane potential is low, JC-1 cannot aggregate in the matrix of mitochondria and produce green fluorescence (ex=488 nm, em= 530 nm) .
ROS inducer 4 (compound TE3) is a mitochondrial inhibitor. ROS inducer 4 causes a series of mitochondria-related physiological changes in tumors, such as mitochondrial fragmentation, explosive generation and accumulation of ROS, decreased mitochondrialmembrane potential, decreased ATP content, and activation of ROS-mediated apoptotic signaling in mitochondria .
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrialADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrialmembranes of rat heart .
MitoPBN is a mitochondria-targeted antioxidant. It accumulates in the mitochondria following the generation of a mitochondrialmembrane potential by succinate, an effect that is blocked by addition of the mitochondrialmembrane potential uncoupler FCCP. MitoPBN inhibits superoxide activation of mitochondrial uncoupling protein 1 (UCP1), UCP2, and UCP3 when used at a concentration of 250 nM in vitro but does not react with superoxide. It traps hydroxyl (IC50=~77 μM) and carbon-centered radicals and inhibits the initiation of lipid peroxidation in isolated bovine heart mitochondria.
BTM-P1 is a polycationic peptide that exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria. BTM-P1 can form ion-permeable channels in the inner mitochondrialmembrane to interfere with mitochondrial energy processes .
MitoTracker Orange CMTMRos is a fluorescent dye that labels mitochondria within live cells utilizing the mitochondrialmembrane potential (Ex/Em: 551/576 nm) .
Miclxin (DS37262926) is a potent inhibitor of mutant β-catenin, involving in Wnt signaling pathway. Miclxin induces β-catenin-dependent apoptosis, leads to severe mitochondrial damage with the loss of mitochondrialmembrane. Miclxin kills tumor via targeting to MIC60, a major components of the mitochondrial contact site and cristae organizing system (MICOS) complex .
Antifungal agent 92 (Compound 21) is a potent antifungal agent with an EC50 of 4.4 μM against Sclerotinia sclerotiorum. Antifungal agent 92 can induce abnormal mitochondrial morphology, loss of mitochondrialmembrane potential, and reactive oxygen species (ROS) accumulation in Sclerotinia sclerotiorum. Antifungal agent 92 is a moderate promiscuous inhibitor of mitochondrial complexes II and III .
9-OxoODE results from oxidation of the allylic hydroxyl of either 9(S)- or 9(R)-HODE. Rabbit reticulocyte plasma and mitochondrialmembranes contain both 9- and 13-oxoODEs, representing about 2% of the total linoleate residues in the membranes. Most of these oxidized linoleate residues are esterified to membrane lipids.
Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrialmembrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri .
Bid BH3 peptide is a small peptide derived from Bid protein that can bind and activate the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and apoptosis. Bid BH3 peptide can be used to study mitochondrial bioenergetics .
Bongkrekic acid-13C28 is the C13 labeled Bongkrekic acid. Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans. Bongkrekic acid specific ligand for mitochondrial adenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport .
d-(KLAKLAK)2, as an antibacterial and anti-tumor polypeptide, is a representative of the antimicrobial peptide group, and also has good anticancer properties. d-(KLAKLAK)2 is able to kill bacteria by damaging their cell membranes, causing cell contents to leak out. d-(KLAKLAK)2 can also inhibit tumor cell proliferation by causing mitochondrial swelling and mitochondrialmembrane destruction, triggering apoptosis (programmed cell death) .
Pipermethystine is an alkaloid that can be isolated from the Kava plant. Pipermethystine decreases HepG2 cell cellular ATP levels, mitochondrialmembrane potential, and induces apoptosis .
Taurodeoxycholate (sodium salt) (Standard) is the analytical standard of Taurodeoxycholate (sodium salt). This product is intended for research and analytical applications. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses
.
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].
Anticancer agent 161 (Compound 3b) is a bioactive alkynol with anti-cancer potential. Anticancer agent 161 can trigger autophagy and mitochondrialmembrane potential depletion .
Anticancer agent 14 is a lead compound (IC50: 0.20 to 0.65 μM) that induces apoptosis, cell cycle arrest, and loss of mitochondrialmembrane potential in breast cancer cells.
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for research and analytical applications. Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrialmembranes of rat heart .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone is orally active against HMGCR mutation and statin caused myopathy . DL-Mevalonolactone induces inflammation and oxidative stress response with decreased mitochondrialmembrane potential (MMP) and induces mitochondrial swelling [2][4].
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrialmembrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
TSPO Ligand-Linker Conjugates 1 contains a ligand for translocator protein (TSPO) and a linker, which is used for the synthesis of mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC can bind the TSPO on the outer mitochondrialmembrane (OMM) of mitochondria and degrades impaired mitochondria and proteins via mitophagy, and improves mitochondrial activity. TSPO Ligand-Linker Conjugates 1 can be used in mitochondrial dysfunction related research, including neurodegenerative diseases, cancer, and diabetes .
1,2-Dipentadecanoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium functions as an activator for the protein kinase C family and is an anionic phospholipid found in mitochondrial and microsomal membranes, playing a crucial role in the composition of lung surfactant, particularly within the membranes of lamellar bodies in the lungs.
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrialmembrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
Dihydrorhodamine 6G (DHR 6G) is the reduced form of Rhodamine 6G, which is used as fluorescent mitochondrial dye. It is nonfluorescent, but it readily enters most of the cells and is oxidized by oxidative species or by cellular redox systems to the fluorescent rhodamine 6G that accumulates in mitochondrialmembranes. Dihydrorhodamine 6G is useful for detecting reactive oxygen species (ROS) including superoxide .
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrialmembrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
BDE 47 (Standard) is the analytical standard of BDE 47. This product is intended for research and analytical applications. BDE 47 targets mitochondria, inhibits mitochondrial oxidative phosphorylation (OXPHOS), decreases mitochondrialmembrane potential (MMP) and induces apoptosis in embryonic cell. BDE 47 induces the generation of ROS, and activates the JNK signaling pathway. BDE 47 exhibits embryonic developmental toxicity in zebrafish .
5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity .
GW604714X is a potent inhibitor of mitochondrial respiration supported by pyruvate but not other substrates. GW604714X is a highly specific mitochondrial pyruvate carrier (MPC) inhibitor with a Ki <0.1 nM. GW604714X also inhibits L-lactate transport by the plasma membrane monocarboxylate transporter (MCT1), but at concentrations more than 4 orders of magnitude greater than the MPC .
P62-mediated mitophagy inducer (PMI) is a P62-mediated mitophagy activator. P62-mediated mitophagy inducer activates mitochondrialautophagy without recruitment of Parkin or collapse of the mitochondrialmembrane potential and remains active in cells lacking a fully functional PINK1/Parkin pathway. P62-mediated mitophagy inducer serves as a pharmacological tool to study the molecular mechanisms of mitosis, avoiding toxicity and some of the non-specific effects associated with the sudden dissipation of mitochondria lacking membrane potential .
TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1,a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94,and disrupts TRAP1 tetramer stability,induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS,disrupts the mitochondrialmembrane potential,and enhances glycolysis metabolism .
PK-10 is a synergistic antibacterial agent of Fluconazole (HY-B0101) and has strong antifungal activity against a variety of Fluconazole-resistant Candida albicans strains. PK-10 combined with Fluconazole can inhibit hyphae formation and induce the accumulation of reactive oxygen species. It further causes damage to mitochondrialmembrane potential, reduces intracellular ATP content, and leads to mitochondrial dysfunction .
BMAP 28, bovine is an antibacterial peptide. BMAP 28, bovine exhibits antimicrobial activity against gram-positive and gram-negative bacteria, by increasing cell membrane permeability, and causing leakage of cell contents. BMAP 28, bovine exhibits cytotoxicity to cancer cells and activated human lymphocytes. BMAP 28, bovine induces apoptosis through depolarization of mitochondrialmembrane potential .
Palmitoleoyl-CoA triammonium is the triammonium salt form of Palmitoleoyl-CoA (HY-137782). Palmitoleoyl-CoA triammonium can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA triammonium induces the cardiac mitochondrialmembrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA triammonium regulates metabolism via allosteric control of AMPK β1-isoforms .
Palmitoleoyl-CoA lithium is the lithium salt form of Palmitoleoyl-CoA (HY-137782). Palmitoleoyl-CoA lithium can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA lithium induces the cardiac mitochondrialmembrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA lithium regulates metabolism via allosteric control of AMPK β1-isoforms .
Hexokinase (ScHEX1) (EC 2.7.1.1) is a glycolytic enzyme hexokinase that is inhibited by n-acetylglucosamine. Inhibition of Hexokinase (ScHEX1) by n-acetylglucosamine leads to its separation from the mitochondrial outer membrane, resulting in activation of NLRP3 inflammasome .
Milatuzumab (hLL1; MEDI-115) is a humanized anti-CD74 monoclonal antibody. CD74, a integral membrane protein, is associated with the promotion of B-cell growth and survival. Milatuzumab causes free radical oxygen generation, and loss of mitochondrialmembrane potential. Milatuzumaba also decreases CD20/CD74 aggregates and cell adhesion, to lead to cell death .
Rhodamine 6G (Standard) is the analytical standard of Rhodamine 6G. This product is intended for research and analytical applications. Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Anticancer agent 204 (Compound 6), a cinnamide fluorinated derivative, possesses anticancer activity. Anticancer agent 204 can arrest the cell cycle of HepG2 cells in the G1 phase and induce apoptosis by reducing the level of mitochondrialmembrane polarization (MMP) .
Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against Staphylococcus aureus. Sideroxylin inhibits ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrialmembrane, the generation of reactive oxygen species (ROS) .
Diphenyl Phosphate inhibits growth and energy metabolism in zebrafish and mice in a sex-specific manner. Diphenyl Phosphate can inhibit the activity of SDH (respiratory complex II), reduce the expression of CPT1 and disrupts the integrity of the mitochondrialmembrane. Diphenyl Phosphate may be used in research on metabolic diseases .
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
Mofarotene (Ro 40-8757), an arotinoid, is anticancer compound. Mofarotene induces apoptosis, associated with mitochondrialmembrane depolarization, activation of caspase-3 and -9, and enhanced production of reactive oxygen species. Mofarotene inhibits hematopoiesis in vitro by inhibiting maturation from primitive progenitor cells .
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrialmembrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells .
A-1208746 is an inhibitor for MCL-1, with a Ki of 0.454 nM. A-1208746 activates caspase-3/-7, induces apoptosis in cell H929, and decreases mitochondrialmembrane potential. A-1208746 synergies with Navitoclax (HY-10087), and can be used in cancer research .
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrialmembrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrialmembrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis .
Ru3 is a poly(ADP-ribose) polymerase 1 inhibitor. Ru3 induces apoptosisin MCF-7 cells by multiple modes, inclusive of inducing DNA damage, suppressing DNA damage repair, disturbing cell cycle distribution, decreasing the mitochondrialmembrane potential, and increasing the intracellular reactive oxygen species levels .
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrialmembrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrialmembrane potential in refractory prostate cancer cells without modulating p53 activity . Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation .
PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrialmembrane potential and induces apoptosis .
Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrialmembrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
2'-epi-2'-O-Acetylthevetin B (GHSC-74) is a cardiac glycoside that can be isolated from the seeds of Cerbera manghas L. 2'-epi-2'-O-Acetylthevetin B inhibits cell viability, induces apoptosis and loss of mitochondrialmembrane potential in HepG2 cells .
Phosphorylethanolamine (Monoaminoethyl phosphate) is a membrane phospholipid and an important precursor of Phosphatidylcholine (HY-B2233B). It is found in most animal tissues and various human extracranial tumors, playing a critical role in membrane integrity, cell division, mitochondrial respiratory function, and more. Studies have shown that changes in the abundance of Phosphorylethanolamine are associated with Alzheimer's disease and Parkinson's disease. Lowering the ratio of Phosphorylethanolamine to Phosphatidylcholine in the liver can improve insulin signaling. Phosphorylethanolamine holds promise for research in the fields of cancer, neurodegenerative disorders, and metabolic diseases .
GL0388 is a Bax activator that results in Bax insertion into mitochondrialmembrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
VK-28, a brain-permeable iron chelator, inhibits both basal and Fe/ascorbate-induced mitochondrialmembrane lipid peroxidation, with an IC50 of 12.7 μM. VK-28 exhibits significant neuroprotective effects on ICV-6-OHDA. VK-28 can be used for the research of Parkinson’s disease and other neurodegenerative diseases .
T-Cadinol is a sesquiterpene isolated from C. sylvestris that exhibits anti-Trypanosoma cruzi activity, with IC50 values of 18.2 μM and 15.8 μM against trypomastigote and amastigote forms, respectively. T-Cadinol can induce mitochondrial damage in parasites, leading to membrane hyperpolarization and decreased levels of reactive oxygen species. T-Cadinol can be used for the research of Chagas disease .
Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity . 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrialmembrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9 . 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration .
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrialmembranes. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrialmembrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
EGFR-IN-119 (Compound 5l) is an inhibitor for EGFR with an IC50 of 84.3 nM. EGFR-IN-119 inhibits the cytotoxicity in lung cancer cell A549 with an IC50 of 1.34 μM. EGFR-IN-119 downregulates the expressions of EGFR, KRAS, and MAP2K genes, exhibits antioxidant activity through reduction of reactive oxygen species (ROS), and hyperpolarizes the mitochondrialmembrane potential .
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function .
Dabuzalgron (Ro 115-1240) hydrochloride is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron hydrochloride protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function .
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrialmembrane potential (MMP) and induces apoptosis .
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrialmembrane potential and induces apoptosis .
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrialmembrane potential .
PT4 is a therapeutic agent against Cutaneous leishmaniasis (CL). PT4 is effective against both species of Leishmania, with IC50s of 125.18 and 233.18 μM for L. amazonensis and L. braziliensis, respectively. PT4 decreases of mitochondrialmembrane potential and increases production of reactive oxygen species, which leads to parasite death. PT4 has a potent in vivo anti-inflammatory activity .
NMK-TD-100 is a modulator for microtubule. NMK-TD-100 binds to tubulin, inhibits the tubulin polymerization with an IC50 of 17.5 µM, inhibits mitosis, and decreases mitochondrialmembrane potential (MMP). NMK-TD-100 inhibits the proliferation of HeLa with an IC50 of 1.42 µM, arrests cell cycle at G2/M phase, induces apoptosis in HeLa .
Ferroptosis/apoptosis inducer-1 (compound 4d) is a dual inducer of apoptosis and ferroptosis. Ferroptosis/apoptosis inducer-1 induces apoptosis and ferroptosis by reducing mitochondrialmembrane potential and downregulating GPX4. Ferroptosis/apoptosis inducer-1 can significantly inhibit the proliferation and metastasis of triple-negative breast cancer (TNBC) both in vitro and in vivo, playing an important role in cancer research .
Bax agonist 1 (compound SMBA2) is a Bax agonist (Ki=57.2 nM). Bax agonist 1 induces Bax conformational changes by blocking S184 phosphorylation, promoting Bax insertion into the mitochondrialmembrane and forming Bax oligomers, which induce cytochrome c release and apoptosis in malignant cancer cells expressing Bax. Bax agonist 1 can be used in lung cancer research .
d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrialmembrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects .
Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrialmembrane potential .
Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings .
Taurodeoxycholic acid-d5is the deuterium labeledTaurodeoxycholic acid(HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrialmembrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
Apoptosis inducer 19 (Compound 7g) is an Apoptosis inducer. Apoptosis inducer 19 elevates expression of pro-apoptotic proteins (Bax and caspase-3) and downregulates anti-apoptotic protein (Bcl-2). Apoptosis inducer 19 upregulates cellular reactive oxygen species (ROS) levels and disrupts mitochondrialmembrane potential (MMP). Apoptosis inducer 19 can be used for triple-negative breast cancer (TNBC) research .
Antitumor agent-182 (Compound 12a) decreases mitochondrialmembrane potential (MMP) and enhances ROS levels. Antitumor agent-182 arrests the cell cycle at G0/G1 phase, induces apoptosis in HeLa. Antitumor agent-182 inhibits the proliferation of HeLa, PC-3 and HCT-15 with IC50s of 8.83, 10.07 and 7.84 μM, respectively .
Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cell cycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrialmembrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4 .
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrialmembrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrialmembrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrialmembrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC50 of 3 μM by using Ba 2+ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrialmembrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells .
Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrialmembrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
Glibenclamide (Standard) is the analytical standard of Glibenclamide. This product is intended for research and analytical applications. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity . 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrialmembrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9 . 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration .
BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrialmembrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
(R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses .
Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrialmembrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrialmembrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research .
Diethyl succinate (Standard) is the analytical standard of Diethyl succinate. This product is intended for research and analytical applications. Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings .
PMMB-187 is a selective STAT3 inhibitor with an IC50 value of 1.81 μM for MDA-MB-231 cells. PMMB-187 induces apoptosis (Apoptosis) in MDA-MB-231 cells by inhibiting STAT3 transcriptional activity, nuclear translocation, and downstream target gene expression, while also reducing mitochondrialmembrane potential, generating reactive oxygen species (ROS), and upregulating the expression levels of apoptosis-related proteins. PMMB-187 has potential applications in cancer research .
Phosphatidylethanolamine is the most abundant phospholipid in prokaryotes and the second most abundant found in the membrane of mammalian, plant, and yeast cells, comprising approximately 25% of total mammalian phospholipids. In the brain, phosphatidylethanolamine comprises almost half of the total phospholipids. It is synthesized mainly through the cytidine diphosphate-ethanolamine and phosphatidylserine decarboxylation pathways, which occur in the endoplasmic reticulum (ER) and mitochondrialmembranes, respectively. It is a precursor in the synthesis of phosphatidylcholine and arachidonoyl ethanolamide and is a source of ethanolamine used in various cellular functions. In E. coli, phosphatidylethanolamine deficiency prevents proper assembly of lactose permease, suggesting a role as a lipid chaperone. It is a cofactor in the propagation of prions in vitro and can convert recombinant mammalian proteins into infectious molecules even in the absence of RNA. This product contains phosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 and sn-2 positions.
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrialmembrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
Deoxyenterocin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibiotic, antiviral, and antioxidant properties. It inhibits the growth of S. lutea, S. aureus, K. pneumoniae, and V. percolans in vitro when used at a concentration of 500 μg/mL. Deoxyenterocin (50 μg/mL) inhibits the cytopathic effect of influenza A H1N1 virus by 60.6% in vitro. It also prevents hydrogen peroxide-induced decreases in glutathione (GSH) levels and in the mitochondrialmembrane potential in mouse primary cortical neuronal cultures when used at a concentration of 1 μM.
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrialmembrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrialmembrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection .
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrialmembrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrialmembrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrialmembrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
Ferroptosis-IN-7(Compound 26) is a ferroptosis inhibitor which can restore cell viability, reduce iron accumulation and scavenge reactive oxygen species. Ferroptosis-IN-7 can be used for vascular diseases research .
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrialmembrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
VEGFR-2-IN-51 (compound 19) is an orally active dual-target inhibitor of VEGFR-2 (IC50=15.33 μM) and tubulin (IC50=0.76 μM) with anti-tumor activity. VEGFR-2-IN-51 induces tumor cell apoptosis by reducing mitochondrialmembrane potential and increasing reactive oxygen species (ROS) levels. VEGFR-2-IN-51 exerts anti-angiogenic effects by blocking the VEGFR-2/PI3K/AKT signaling pathway. In addition, VEGFR-2-IN-51 has significant anti-proliferative activity against the gastric cancer cell line MGC-803 (IC50=0.005 μM) .
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrialmembrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrialmembrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Normal mitochondrial function is critical for maintaining cellular homeostasis because mitochondria produce ATP and are the major intracellular source of free radicals. Cellular dysfunctions induced by intracellular or extracellular insults converge on mitochondria and induce a sudden increase in permeability on the inner mitochondrialmembrane, the so-called mitochondrialmembrane permeability transition (MMPT). MMPT is caused by the opening of pores in the inner mitochondrialmembrane, matrix swelling, and outer membrane rupture. The MMPT is an endpoint to initiate cell death because the pore opening together with the release of mitochondrial cytochrome c activates the apoptotic pathway of caspases.
The normal operation of mitochondrial function is important for maintaining normal cell death and treatment of mitochondrial diseases. MCE offers a unique collection of 627 compounds with identified and potential mitochondrial protective activity. MCE Mitochondrial Protection Compound Library is critical for drug discovery and development.
DiSC3(5) is a fluorescent probe commonly used as a tracer dye to evaluate mitochondrialmembrane potential. The excitation/emission wavelength of DiSC3(5) is up to 622/670 nm. DiSC3(5) can inhibit the respiratory system associated with mitochondrial NAD, and the IC50 value is 8 μM. DiSC3(5) in the presence of Na +/K +-ATPase inhibitor ouabain 2 can induce membrane hyperpolarization of Ehrlich ascites tumor cells .
Mito-Tracker Green is a green fluorescent dye that selectively accumulates in the mitochondrial matrix. MitoTracker Green FM covalently binds mitochondrial proteins by reacting with free mercaptan of cysteine residues, allowing staining of mitochondrialmembrane potential independent of membrane potential. Excitation/emission wavelength 490/523 nm.
JC-1 (CBIC2) is an ideal fluorescent probe widely used to detect mitochondrialmembrane potential. JC-1 accumulates in mitochondria in a potential dependent manner and can be used to detect the membrane potential of cells, tissues or purified mitochondria. In normal mitochondria, JC-1 aggregates in the mitochondrial matrix to form a polymer, which emits strong red fluorescence (Ex=488 nm, Em=595 nm); When the mitochondrialmembrane potential is low, JC-1 cannot aggregate in the matrix of mitochondria and produce green fluorescence (ex=488 nm, em= 530 nm) .
MitoTracker Orange CMTMRos is a fluorescent dye that labels mitochondria within live cells utilizing the mitochondrialmembrane potential (Ex/Em: 551/576 nm) .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
HBmito Crimson is a deep red fluorescent probe (λex: 658 nm, λem: 678 nm) for the inner mitochondrialmembrane. HBmito Crimson is a cell membrane-permeable probe with high selectivity for the mitochondrial inner membrane, suitable for specific fluorescence staining of the inner mitochondrialmembrane in living cells. HBmito Crimson has high photostability and brightness, suitable for long-term dynamic fluorescence imaging.
Mito Red is a vital dye and mitochondrial stain that can be used to detect and evaluate mitochondrial function and status. Mito Red accumulates in mitochondria, and its fluorescence intensity is positively correlated with mitochondrialmembrane potential. When the mitochondrialmembrane potential increases, the fluorescence signal of Mito Red increases .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
Rhodamine 6G (Standard) is the analytical standard of Rhodamine 6G. This product is intended for research and analytical applications. Rhodamine dyes are membrane-permeable cationic fluorescent probes that specifically recognize mitochondrialmembrane potentials, thereby attaching to mitochondria and producing bright fluorescence, and at certain concentrations, rhodamine dyes have low toxicity to cells, so they are commonly used to detect mitochondria in animal cells, plant cells, and microorganisms .
POPSO is a zwitterionic buffer, increases osmolality and shows marked inhibition of anion uniport. POPSO inhibits chloride uniport with an IC50 value of 24 mM. POPSO enhances copper uptake and toxicity in alga, impairs mitochondrial inner membrane. The working pH range of POPSO sesquisodium salt is 7.2-8.5 .
S-15176 difumarate is a compound with the activity of regulating mitochondrialmembrane potential. S-15176 difumarate can act on the inner mitochondrialmembrane to change the mitochondrialmembrane potential.
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrialmembrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
KLA peptide is a biological active peptide. (a cationic amphipathic mitochondrialmembrane disrupting peptide that induces programmed cell death by disrupting mitochondrialmembrane, but cannot cross the plasma
membrane)
Pezadeftide is a potent antifungal peptide. Pezadeftide can enter fungal cells and cause a rapid mitochondrial response that results in hyperpolarization of the mitochondrialmembrane .
BTM-P1 is a polycationic peptide that exhibits antibacterial activity against both Gram-positive and Gram-negative bacteria. BTM-P1 can form ion-permeable channels in the inner mitochondrialmembrane to interfere with mitochondrial energy processes .
Bid BH3 peptide is a small peptide derived from Bid protein that can bind and activate the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and apoptosis. Bid BH3 peptide can be used to study mitochondrial bioenergetics .
d-(KLAKLAK)2, as an antibacterial and anti-tumor polypeptide, is a representative of the antimicrobial peptide group, and also has good anticancer properties. d-(KLAKLAK)2 is able to kill bacteria by damaging their cell membranes, causing cell contents to leak out. d-(KLAKLAK)2 can also inhibit tumor cell proliferation by causing mitochondrial swelling and mitochondrialmembrane destruction, triggering apoptosis (programmed cell death) .
Smac-N7 peptide, the seven N-terminal amino acid of the mitochondrial protein Smac (second mitochondria-derived activator of caspase), cannot pass through the cell membrane .
BMAP 28, bovine is an antibacterial peptide. BMAP 28, bovine exhibits antimicrobial activity against gram-positive and gram-negative bacteria, by increasing cell membrane permeability, and causing leakage of cell contents. BMAP 28, bovine exhibits cytotoxicity to cancer cells and activated human lymphocytes. BMAP 28, bovine induces apoptosis through depolarization of mitochondrialmembrane potential .
d-KLA Peptide is a synthetic pro-apoptotic peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrialmembrane. d-KLA Peptide activates biochemical pathways associated with apoptosis, including the activation of caspase family proteins and PARP (poly ADP ribose polymerase). d-KLA Peptide can be used to carry and deliver genes or small molecules to enhance anti-tumor effects .
Bid BH3 (80-99) is a biological active peptide. (BID is a pro-apoptotic member of the 'BH3-only' (BOPS) subset of the BCL-2 family of proteins that constitute a critical control point in apoptosis. Bid is the first of the BOPs reported to bind and activate Bcl-2, Bax, and Bak. Bid serves as a death-inducing ligand that moves from the cytosol to the mitochondrialmembrane to inactivate Bcl-2 or to activate Bax.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
MCE JC-1 MitochondrialMembrane Potential Assay Kit uses JC-1 to detect the mitochondrialmembrane potential in variety of cell types, as well as intact tissues and isolated mitochondria.
Milatuzumab (hLL1; MEDI-115) is a humanized anti-CD74 monoclonal antibody. CD74, a integral membrane protein, is associated with the promotion of B-cell growth and survival. Milatuzumab causes free radical oxygen generation, and loss of mitochondrialmembrane potential. Milatuzumaba also decreases CD20/CD74 aggregates and cell adhesion, to lead to cell death .
Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses
.
Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrialADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrialmembranes of rat heart .
DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone is orally active against HMGCR mutation and statin caused myopathy . DL-Mevalonolactone induces inflammation and oxidative stress response with decreased mitochondrialmembrane potential (MMP) and induces mitochondrial swelling [2][4].
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrialmembrane potential .
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrialmembrane depolarization .
Pipermethystine is an alkaloid that can be isolated from the Kava plant. Pipermethystine decreases HepG2 cell cellular ATP levels, mitochondrialmembrane potential, and induces apoptosis .
Taurodeoxycholate (sodium salt) (Standard) is the analytical standard of Taurodeoxycholate (sodium salt). This product is intended for research and analytical applications. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses
.
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for research and analytical applications. Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrialmembranes of rat heart .
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrialmembrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against Staphylococcus aureus. Sideroxylin inhibits ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrialmembrane, the generation of reactive oxygen species (ROS) .
Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrialmembrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
2'-epi-2'-O-Acetylthevetin B (GHSC-74) is a cardiac glycoside that can be isolated from the seeds of Cerbera manghas L. 2'-epi-2'-O-Acetylthevetin B inhibits cell viability, induces apoptosis and loss of mitochondrialmembrane potential in HepG2 cells .
Phosphorylethanolamine (Monoaminoethyl phosphate) is a membrane phospholipid and an important precursor of Phosphatidylcholine (HY-B2233B). It is found in most animal tissues and various human extracranial tumors, playing a critical role in membrane integrity, cell division, mitochondrial respiratory function, and more. Studies have shown that changes in the abundance of Phosphorylethanolamine are associated with Alzheimer's disease and Parkinson's disease. Lowering the ratio of Phosphorylethanolamine to Phosphatidylcholine in the liver can improve insulin signaling. Phosphorylethanolamine holds promise for research in the fields of cancer, neurodegenerative disorders, and metabolic diseases .
T-Cadinol is a sesquiterpene isolated from C. sylvestris that exhibits anti-Trypanosoma cruzi activity, with IC50 values of 18.2 μM and 15.8 μM against trypomastigote and amastigote forms, respectively. T-Cadinol can induce mitochondrial damage in parasites, leading to membrane hyperpolarization and decreased levels of reactive oxygen species. T-Cadinol can be used for the research of Chagas disease .
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity . 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrialmembrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9 . 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration .
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrialmembrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings .
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrialmembrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .
2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity . 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrialmembrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9 . 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration .
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
(R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses .
Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrialmembrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Diethyl succinate (Standard) is the analytical standard of Diethyl succinate. This product is intended for research and analytical applications. Diethyl succinate (Diethyl Butanedioate) can be utilized at physiological pH, allowing it to penetrate biological membranes and integrate into the cells of tissue cultures, where it is metabolized via the tricarboxylic acid cycle. Diethyl succinate modulates the polarization and activation of microglial cells by reducing mitochondrial fission and the levels of reactive oxygen species (ROS), thereby exerting an inflammatory protective effect in primary microglial cells. Furthermore, Diethyl succinate is non-toxic and can be used in flavorings and seasonings .
Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrialmembrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury .
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrialmembrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
Guaiol (Standard) is the analytical standard of Guaiol. This product is intended for research and analytical applications. Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions [4]
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrialmembrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
ATP5J2 protein is a component of mitochondrial membrane ATP synthase (complex V), which uses the proton gradient established by the respiratory chain electron transport complex to help ADP synthesize ATP. ATP5J2 is located in the F(0) domain as a small subunit and cooperates with subunit a in the membrane. ATP5J2 Protein, Human (Cell-Free, His) is the recombinant human-derived ATP5J2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of ATP5J2 Protein, Human (Cell-Free, His) is 94 a.a., with molecular weight of 12.4 kDa.
The TIM-14 protein is an important component of the PAM complex and is required for the transport of transit peptide-containing proteins from the inner membrane to the mitochondrial matrix using ATP. TIM-14 Protein, S.cerevisiae is the recombinant TIM-14 protein, expressed by E. coli , with tag free. The total length of TIM-14 Protein, S.cerevisiae is 70 a.a., with molecular weight of ~9.0 kDa.
TIM-16 protein is an important component of the PAM complex, which uses ATP to promote the transfer of transit peptide-containing proteins from the inner membrane to the mitochondrial matrix. TIM-16 Protein, S. cerevisiae is the recombinant TIM-16 protein, expressed by E. coli , with tag free. The total length of TIM-16 Protein, S. cerevisiae is 66 a.a., with molecular weight of ~11.0 kDa.
ATP5MG Protein, an essential part of mitochondrial membrane ATP synthase (Complex V), facilitates ATP generation from ADP using the proton gradient established by respiratory chain electron transport complexes. Positioned within the F(0) domain as a minor subunit alongside subunit a, ATP5MG collaborates with various subunits in the overall F-type ATPase complex, including CF(1) and CF(0), to ensure efficient ATP synthesis. ATP5MG Protein, Bovine (Myc, His) is the recombinant bovine-derived ATP5MG protein, expressed by E. coli , with N-His, C-Myc labeled tag.
CYB5B Protein, Human (HEK293, His) is the recombinant human-derived CYB5B protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CYB5B Protein, Human (HEK293, His) is 107 a.a., with molecular weight of ~22.0 kDa.
SLC25A46 is a mitochondrial outer membrane transmembrane protein that critically regulates mitochondrial organization by affecting the MICOS complex and participating in mitochondrial cristae biogenesis. Its association with EMC suggests involvement in mitochondrial lipid homeostasis and fission. SLC25A46 Protein, Human (Sf9, His, MBP, FLAG) is the recombinant human-derived SLC25A46 protein, expressed by Sf9 insect cells , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC25A46 Protein, Human (Sf9, His, MBP, FLAG) is 417 a.a., .
Bongkrekic acid-13C28 is the C13 labeled Bongkrekic acid. Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans. Bongkrekic acid specific ligand for mitochondrial adenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport .
DL-Mevalonolactone-d7 is the deuterium labeled DL-Mevalonolactone. DL-Mevalonolactone ((±)-Mevalonolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrialmembrane potential (∆Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[1][2].
Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
Taurodeoxycholate-d6 (sodium salt) is the deuterium labeled Taurodeoxycholate sodium salt[1]. Taurodeoxycholate sodium salt is a bile salt-related anionic detergent used for isolation of membrane proteins including inner mitochondrialmembrane proteins. Taurodeoxycholate (TDCA) inhibits various inflammatory responses[2]. [2][3].
DL-Mevalonolactone-d3 is the deuterium labeled DL-Mevalonolactone[1]. DL-Mevalonolactone ((±)-Mevalonolactone;Mevalolactone) is the δ-lactone form of mevalonic acid, a precursor in the mevalonate pathway. DL-Mevalonolactone (Mevalonolactone) decreases mitochondrialmembrane potential ( Ψm), NAD(P)H content and the capacity to retain Ca2+ in the brain, besides inducing mitochondrial swelling[2][3].
Taurodeoxycholic acid-d5is the deuterium labeledTaurodeoxycholic acid(HY-B1899) . Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrialmembrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD) .
Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
TOMM20 Antibody (YA1380) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1380), targeting TOMM20, with a predicted molecular weight of 16 kDa (observed band size: 16 kDa). TOMM20 Antibody (YA1380) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human, hamster background.
Alkyne-phenol (Alk-Ph) is a clickable ascorbate peroxidase 2 (APEX2) probe. Alkyne-phenol substantially improves APEX-labeling efficiency in intact yeast cells, as it is more cell wall-permeant than APEX2 substrate biotin-phenol (BP). Alkyne-phenol also facilitates the identification of APEX-labeling sites, allowing the unambiguous assignment of membrane topology of mitochondrial proteins . Alkyne-phenol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Photoclick cholesterol is a sterol lipid cholesterol analog that contains a clickable terminal alkyne moiety and a photoactivatable diaziridine group. Photoclick cholesterol has the ability to photoaffinity label the mitochondrial outer membrane transport protein (TSPO) and is able to specifically bind cholesterol to TSPO. However, using excessive amounts of Photoclick cholesterol will reduce the photolabeling of total mitochondrial proteins and TSPO .
18:0 Cardiolipin (CL) is a polyglycerophospholipid synthesized in mitochondria, playing a crucial role in mitochondrial bioenergetics and signaling. Exclusively found in the inner mitochondrialmembrane of eukaryotes, 18:0 CL exhibits a complex structure characterized by its unique chain length and degree of saturation, along with the specific arrangements of its four fatty acid substituents.
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