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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
509 Results for "
membrane potential
" in MedChemExpress (MCE) Product Catalog:
Products (509)
509 Results for "membrane potential" in MCE Product Catalog:
Synonyms: DiMC; CHC 004; Di-O-methylcurcumin
Target:
Androgen Receptor Reactive Oxygen Species (ROS) Apoptosis NF-κB CDK Fatty Acid Synthase (FASN) Acetyl-CoA Carboxylase PI3K Akt AMPK ERK JNK
Research Areas:
Dimethoxycurcumin (DiMC) is a curcuminoid compound found in Curcuma longa. Dimethoxycurcumin is also an orally active thioredoxin reductase inhibitor (IC50 = 5.4 μM) and androgen receptor antagonist. Dimethoxycurcumin inhibits thioredoxin reductase, leading to oxidized thioredoxin accumulation, ROS production, DNA damage, glutathione depletion, mitochondrial membrane potential decrease, ATP depletion, S phase arrest, and apoptosis. Dimethoxycurcumin inhibits NF-κB, NADPH oxidase subunits, ATP synthase subunits, CDK4, cyclin-D1, FASN, ACC, and the IRS2-PI3K-Akt pathway, while activating AMPK, ERK, and JNK. Dimethoxycurcumin can be used for research on cancer, arsenic-induced hepatotoxicity, and tuberculosis .
Cat. No.: HY-109566R
CAS No.: 2089288-03-7
Synonyms: AZD1390 (Standard)
Research Areas:
Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC50 values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer .
Research Areas:
PROTAC α-synuclein degrader 5 is a selective PROTAC degrader targeting α‑synuclein aggregates, with a DC50 of 7.51 μM. PROTAC α-synuclein degrader 5 binds to αSyn aggregates, recruits the CRBN E3 ubiquitin ligase, and mediates the ubiquitination and subsequent degradation of α‑synuclein aggregates. PROTAC α-synuclein degrader 5 activates the autophagy-lysosome pathway. PROTAC α-synuclein degrader 5 reduces ROS levels in neuroblastoma cells, restores mitochondrial membrane potential, rescues cell viability, and decreases LDH release. PROTAC α-synuclein degrader 5 degrades αSyn aggregates in Caenorhabditis elegans and ameliorates oxidative stress. PROTAC α-synuclein degrader 5 is used for the research of synucleinopathies, such as Parkinson's disease .
Cat. No.: HY-159510
Research Areas:
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 mitochondrial membrane 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) .
Cat. No.: HY-16958R
CAS No.: 72596-74-8
Research Areas:
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 mitochondrial membrane 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 .
Cat. No.: HY-178967
Research Areas:
DRAK1/2-IN-2 (Compound Y17) is a DRAK1/2 inhibitor with IC50 values for DRAK2 and DRAK1 of 353.2 nM and 507.4 nM respectively. DRAK1/2-IN-2 can enhance mitochondrial membrane potential and glucose-stimulated insulin secretion (GSIS). DRAK1/2-IN-2 resists lipotoxicity-induced cell apoptosis. DRAK1/2-IN-2 significantly inhibits the secretion of pro-inflammatory cytokine IL-1β, thereby exerting an anti-inflammatory effect. DRAK1/2-IN-2 can significantly lower the blood glucose levels of mice. DRAK1/2-IN-2 can be used in diabetes research.
Cat. No.: HY-180292
CAS No.: 2882998-56-1
Research Areas:
Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma .
Cat. No.: HY-183327
Target:
PI3K mTOR Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism Bcl-2 Family Caspase
Research Areas:
PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models .
Cat. No.: HY-187191
Target:
Glutathione Peroxidase Akt EGFR Reactive Oxygen Species (ROS) Ferroptosis Apoptosis Autophagy
Research Areas:
Autophagy-IN/Ferroptosis inducer-modulator-1 is a dual-functional molecule that acts as an Autophagy inhibitor and a Ferroptosis inducer. Autophagy-IN/Ferroptosis inducer-modulator-1 downregulates GPX4 expression, elevates ROS levels and reduces mitochondrial membrane potential. Autophagy-IN/Ferroptosis inducer-modulator-1 arrests the cell cycle of non-small cell lung cancer (NSCLC) cells, induces mild apoptosis and inhibits autophagy. Autophagy inhibition induced by Autophagy-IN/Ferroptosis inducer-modulator-1 acts upstream of ferroptosis to produce a synergistic effect. Autophagy-IN/Ferroptosis inducer-modulator-1 exhibits anti-tumor activity against both human tumor cells and zebrafish xenograft models. Autophagy-IN/Ferroptosis inducer-modulator-1 can be used for research related to non-small cell lung cancer .
Cat. No.: HY-19882
CAS No.: 941285-15-0
BAL-30072 is a siderophore-bearing monocyclic β-lactam antibiotic with antibacterial activity. BAL-30072 inhibits penicillin-binding proteins 1a, 1b, and 3, thereby disrupting bacterial cell wall synthesis. BAL-30072 inhibits mitochondrial electron transport chain complex II and complex III, while also inhibiting glycolysis and mitochondrial fatty acid β-oxidation. BAL-30072 induces mitochondrial ROS production, cellular ATP depletion, reduces mitochondrial membrane potential, and triggers hepatocyte apoptosis via caspase-3/7 activation. BAL-30072 is a substrate of the hepatic uptake transporters OAT1 and OAT3. BAL-30072 can be used in research related to bacterial infections .
Cat. No.: HY-N3584R
CAS No.: 68124-04-9
Synonyms: Chonglou Saponin VII (Standard)
Cat. No.: HY-N6784
CAS No.: 11050-94-5
Target:
Cat. No.: HY-N6812
CAS No.: 39089-30-0
Cat. No.: HY-P1723A
Synonyms: Neuropeptide Q TFA
Research Areas:
Cat. No.: HY-W709349
CAS No.: 33400-45-2
Synonyms: D 9998 hydrochloride
Target:
Research Areas:
Flupirtine (D 9998) hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
Cat. No.: HY-L938
8350 compounds
Currently,the incidence and mortality rates of clinical fungal infections remain high. Existing antifungal drugs are limited in variety and associated with numerous adverse effects, creating an urgent demand for the development of novel antifungal agents. Antifungal compound libraries can support the screening and development of new antifungal drugs.
The mechanisms of action of antifungal drugs cover key processes such as fungal cell membrane synthesis, cell wall synthesis, and cell division. They exert fungicidal or fungistatic effects by specifically targeting different molecular pathways. This library includes a variety of core analogs of antifungal drugs, making it adaptable to antifungal research in diverse scenarios. It can be used for the high-throughput screening of novel antifungal drug candidates, enabling the rapid identification of compounds with potential antifungal activity and facilitating the elucidation of drug-target interactions and resistance mechanisms. Additionally, it supports the screening of compounds and combinations that reverse drug resistance, thereby uncovering the novel antifungal potential of existing compounds.
The library comprises 8350 compounds with a well-defined screening strategy. The core sources of the compounds include analogs of known antifungal active moleculeswith a similarity score of ≥ 0.6 MCE has collected more than 500 antifungal molecules.All screened compounds conform to lead-like physicochemical properties, exhibiting both structural diversity and drug-like characteristics, and providing valuable support for the research and development of novel antifungal drugs.
Cat. No.: HY-110230
CAS No.: 1324717-75-0
Synonyms: D 9998-d4 hydrochloride
Research Areas:
Flupirtine-d4 (D 9998-d4) hydrochloride is the deuterium labeled Flupirtine hydrochloride (HY-W709349). Flupirtine hydrochloride is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine hydrochloride is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine hydrochloride stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine hydrochloride exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine hydrochloride functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine hydrochloride can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
Cat. No.: HY-155064
CAS No.: 3031102-92-5
Target:
Research Areas:
TRAP1-IN-2 is a TRAP1-selective inhibitor, with a Kd value of 0.04 μM against human TRAP1. TRAP1-IN-2 exhibits more than 250-fold selectivity for Grp94 and shows no detectable affinity for cytosolic Hsp90α/β. TRAP1-IN-2 selectively induces the degradation of TRAP1 client proteins by inhibiting its ATPase activity, without triggering the heat shock response or affecting cytosolic Hsp90 client proteins. TRAP1-IN-2 suppresses oxidative phosphorylation, shifts cellular metabolism toward glycolysis, disrupts the stability of the TRAP1 tetramer and the mitochondrial membrane potential. TRAP1-IN-2 can be used in studies related to prostate cancer, cervical cancer, and ovarian cancer .
Cat. No.: HY-159122
CAS No.: 3009842-92-3
Research Areas:
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 mitochondrial membrane 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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
