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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
222 Results for "
depolarization
" in MedChemExpress (MCE) Product Catalog:
Products (222)
222 Results for "depolarization" in MCE Product Catalog:
Cat. No.: HY-184214
Research Areas:
Antileishmanial agent-44 is a histone deacetylase inhibitor targeting Leishmania donovani Sir2, with an IC50 of 0.652 μM against amastigotes. Antileishmanial agent-44 elevates ROS levels to induce oxidative stress, which causes mitochondrial membrane potential depolarization, cytochrome c release, phosphatidylserine externalization and DNA fragmentation, triggers apoptosis-like cell death, and arrests the cell cycle. Antileishmanial agent-44 upregulates the expression of Th1-type cytokines and NO in macrophages, reshapes host immune responses to eliminate intracellular parasites. Antileishmanial agent-44 inhibits parasites in infected golden hamsters in vivo. Antileishmanial agent-44 can be used for the research of visceral leishmaniasis.
Cat. No.: HY-184557
CAS No.: 2223036-84-6
Research Areas:
DZ-1-DHA is a conjugate of DHA (HY-B2167) and DZ-1 dye. DZ-1-DHA mediates selective cellular uptake via binding to overexpressed OATP1A2. DZ-1-DHA induces the cleavage of Caspase-3, Caspase-8, Caspase-9 and PARP-1. DZ-1-DHA induces Apoptosis and Ferroptosis. DZ-1-DHA induces ROS production through a Fenton-like mechanism, causes mitochondrial membrane depolarization, and triggers lipid peroxidation. DZ-1-DHA can be used in studies related to colorectal cancer liver metastasis .
Cat. No.: HY-187518
CAS No.: 3134912-65-2
Target:
Research Areas:
NMT-IN-9 is an arylpyrrolidone-based NMT inhibitor with an IC50 of 93.20 nM and a KD of 5.57 × 10 -9 M against NMT. NMT-IN-9 exhibits broad-spectrum antifungal activity against Candida albicans, Candida glabrata, Candida tropicalis, Cryptococcus neoformans and Aspergillus fumigatus, with an MIC of 2-16 μg/mL, and retains activity against fluconazole-resistant Candida isolates, with an MIC of 8-16 μg/mL. NMT-IN-9 induces intracellular ROS accumulation, mitochondrial membrane depolarization, DNA damage, apoptosis and necrotic cell death in fungal cells, and disrupts fungal cell integrity. NMT-IN-9 can be used for studies on NMT-targeted antifungal mechanisms and fluconazole-resistant Candida infections .
Research Areas:
F16 is a mitochondrial permeability transition pore (PTP) modulator with an EC50 of 30 μM in mice. F16 promotes PTP opening, accumulates in cancer cell mitochondria, and induces mitochondrial depolarization, swelling, cristae disruption, outer membrane rupture, ATP depletion, reactive oxygen species (ROS) production, cytochrome c release and mitochondrial uncoupling. F16 induces cell cycle arrest at the G1 (occasionally G2) phase, reduces the phosphotyrosine content of Neu, as well as the levels of phosphorylated PKB/Akt and phosphorylated MAP kinase, downregulates the protein expression levels of Neu and PKB, triggers apoptosis in cells with moderate Bcl-2 expression, and induces necrosis in cells with overexpressed Bcl-2. F16 can be used in research related to breast cancer and gastric cancer .
Cat. No.: HY-132184S
CAS No.: 1881277-30-0
Synonyms: 5,6-EET-d11; (±)5,6-EpETrE-d11
Cat. No.: HY-174374
CAS No.: 3076446-44-8
Target:
Research Areas:
Topobexin is a TOP2B-selective inhibitor with IC50 values of 0.19 μM and 4.8 μM for TOP2B and TOP2A (DNA decatenation assay). Topobexin binds to non-homologous residues in the obex pocket and targets the ATPase domain of TOP2B. Topobexin prevents anthracycline-induced DNA double-strand break formation, apoptotic signaling mediated by caspase 3/7, 8 and 9, cardiomyocyte morphological changes, mitochondrial depolarization/loss, left ventricular systolic dysfunction, extracellular matrix remodeling, fibrotic alterations, and increases in plasma cardiac troponin T and BNP. Topobexin does not impair the antiproliferative effects of anthracyclines in cancer cells, exhibits no intrinsic cytotoxicity in cardiomyocytes, and is well tolerated in rabbits. Topobexin can be used in studies related to anthracycline-induced cardiotoxicity .
Cat. No.: HY-184291
CAS No.: 3114314-82-5
Research Areas:
VCP/p97 IN-4 is a p97/VCP inhibitor (Kd=14.99 μM) targeting the allosteric site of the D1-D2 domain. VCP/p97 IN-4 inhibits the ATPase activity of VCP/p97 in an ATP concentration-independent manner. VCP/p97 IN-4 induces apoptosis, autophagy, mitochondrial stress and mitochondrial membrane depolarization. VCP/p97 IN-4 inhibits the growth of patient-derived colorectal cancer organoids and exhibits in vivo efficacy in a colorectal cancer xenograft mouse model. VCP/p97 IN-4 can be used for the research of colorectal cancer .
Cat. No.: HY-34464
CAS No.: 136630-39-2
Synonyms: 2,7-DBCZ
Research Areas:
2,7-Dibromocarbazole (2,7-DBCZ) is an orally active AhR agonist and MAOB inhibitor that can cross the blood-brain barrier. 2,7-Dibromocarbazole induces CYP1A/CYP1B1, developmental toxicity and oxidative toxicity, Akt phosphorylation, apoptosis, mitochondrial depolarization, and calcium elevation. 2,7-Dibromocarbazole disrupts dopamine homeostasis, promotes α-synuclein aggregation and transcriptomic dysregulation, leading to hepatic lipid accumulation, liver lesions, brain injury, and angiogenesis/energy metabolism disorders, while activating ERα and inhibiting GRα. 2,7-Dibromocarbazole can be used in research on cardiotoxicity and Parkinson's disease .
Cat. No.: HY-N16771
CAS No.: 28384-44-3
Target:
Cat. No.: HY-N6663R
CAS No.: 13466-78-9
Cat. No.: HY-W017424R
CAS No.: 136-95-8
Research Areas:
2-Aminobenzothiazole (Standard) is the analytical standard of 2-Aminobenzothiazole. This product is intended for research and analytical applications. 2-Aminobenzothiazole acts as a caspase 3/7 activator, an anticancer cytotoxic agent, and also exhibits neurotoxicity. 2-Aminobenzothiazole drives the apoptotic pathway by activating caspase 3/7, induces mitochondrial inner membrane depolarization, and triggers both early and late apoptosis via a caspase-dependent pathway. In zebrafish models, 2-Aminobenzothiazole induces oxidative damage in brain tissues and inhibits genes related to GABA and 5-HT synthesis pathways. Long-term exposure to 2-Aminobenzothiazole impairs motor ability, social behavior, anxiety-like state and cognitive function. 2-Aminobenzothiazole can be used in studies of human laryngeal carcinoma and related neurotoxicity .
Cat. No.: HY-123320S
Target:
Research Areas:
MFN2 agonist-1 is an allosteric agonist of mitofusin 2 (MFN2) with an EC50 of 3 nM. MFN2 agonist-1 mimics the MFN2 HR1 peptide to compete for HR2, disrupt the HR1-HR2 autoinhibitory interaction, stabilize the open conformation of MFN2, and promote GTP hydrolysis and mitochondrial fusion. MFN2 agonist-1 acts in a manner dependent on endogenous MFN1 or MFN2, and does not impair cell viability. MFN2 agonist-1 reverses mitochondrial fragmentation, depolarization, aggregation and axonal transport defects, restores bidirectional movement and improves enhanced autophagy. MFN2 agonist-1 is used in studies related to Charcot-Marie-Tooth disease type 2A, Alzheimer's disease, Parkinson's disease and Huntington's disease .
Cat. No.: HY-173007
CAS No.: 3050831-84-7
Research Areas:
ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids .
Cat. No.: HY-179452
Target:
Research Areas:
KRAS G13D-IN-2 (compound 8B) is a potent orally active KRAS G13D inhibitor with IC50 values of 1.95 μM (HCT-116 G13D) and 2.16 μM (HCT-15 G13D). KRAS G13D-IN-2 induces G1-phase arrest and mitochondrial membrane depolarization. KRAS G13D-IN-2 induces senescence through CDK6/TWIST1 inhibition. KRAS G13D-IN-2 inhibits tumor growth in murine models. KRAS G13D-IN-2 can be used for KRAS G13D-mutant colorectal cancer research .
Cat. No.: HY-P11615
Cat. No.: HY-100395R
CAS No.: 36098-33-6
Target:
Reference Standards Mitochondrial Metabolism Reactive Oxygen Species (ROS) Akt p38 MAPK Bcl-2 Family Apoptosis
Research Areas:
F16 (Standard) is the analytical standard of F16 (HY-100395). This product is intended for research and analytical applications. F16 is a mitochondrial permeability transition pore (PTP) modulator with an EC50 of 30 μM in mice. F16 promotes PTP opening, accumulates in cancer cell mitochondria, and induces mitochondrial depolarization, swelling, cristae disruption, outer membrane rupture, ATP depletion, reactive oxygen species (ROS) production, cytochrome c release and mitochondrial uncoupling. F16 induces cell cycle arrest at the G1 (occasionally G2) phase, reduces the phosphotyrosine content of Neu, as well as the levels of phosphorylated PKB/Akt and phosphorylated MAP kinase, downregulates the protein expression levels of Neu and PKB, triggers apoptosis in cells with moderate Bcl-2 expression, and induces necrosis in cells with overexpressed Bcl-2. F16 can be used in research related to breast cancer and gastric cancer .
Cat. No.: HY-183393
CAS No.: 1798292-13-3
NVP-BHS345 is an ATP-competitive TORC1/TORC2 inhibitor with an IC50 of 1 μM for both targets in yeast. NVP-BHS345 acutely inhibits TORC1/TORC2 kinase activity, even in genetically engineered TOR1 M2282T Saccharomyces cerevisiae strains. NVP-BHS345 also reduces the phosphorylation levels of Ser-232/Ser-233 sites in Sch9, Ypk1/Ypk2 and Rps6, and induces hyperphosphorylation of Slt2 and activation of the cell wall integrity pathway. NVP-BHS345 causes depolarization of the actin cytoskeleton, blocks fluid-phase endocytosis, prevents the accumulation of vacuolar lipophilic dyes, and regulates the phosphorylation levels of Ent1, Pan1, Prk1, Akl1 and other cellular proteins .
Cat. No.: HY-184737
Target:
Drug Derivative Bcl-2 Family Caspase PARP Mitochondrial Metabolism ATP Synthase Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
TPP-C8-CO-DSG bromide is a derivative of Diosgenin (HY-N0177) and an anticancer agent. TPP-C8-CO-DSG bromide downregulates Bcl-2 expression and upregulates Bax expression. TPP-C8-CO-DSG bromide promotes the cleavage of Caspase 9, Caspase 3 and PARP-1. TPP-C8-CO-DSG bromide depolarizes mitochondrial membrane potential, reduces intracellular ATP production, and induces intracellular ROS accumulation. TPP-C8-CO-DSG bromide promotes Apoptosis. TPP-C8-CO-DSG bromide exhibits anticancer activity against prostate cancer, breast cancer, lung adenocarcinoma, cervical cancer and colorectal cancer. TPP-C8-CO-DSG bromide can be used in the research of cervical cancer .
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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
