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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
510 Results for "
localization
" in MedChemExpress (MCE) Product Catalog:
Products (510)
510 Results for "localization" in MCE Product Catalog:
Cat. No.: HY-125535
CAS No.: 1290069-19-0
Domaines de recherche:
OSU-53 is an orally active AMPK activator and mTOR inhibitor, with an IC50 of 0.3 μM for AMPK, an EC50 of 2-5 μM for AMPK, and an IC50 of 8.23 μM for mTOR. OSU-53 inhibits the Akt signaling pathway, directly activates AMPK by binding to its autoinhibitory domain, reduces IKKβ-mediated phosphorylation of Foxo3a, blocks Akt-mediated phosphorylation of MDM2, and promotes the nuclear localization and stabilization of Foxo3a, while directly inhibiting mTOR. OSU-53 inhibits epithelial-mesenchymal transition (EMT), induces epithelial phenotype, suppresses invasion and metastasis, induces autophagy, inhibits the activation of ERK and Akt, reduces the secretion of nitric oxide and proinflammatory cytokines, and inhibits the migration of MDSC; at high doses, it induces MDSC apoptosis, attenuates the immunosuppressive effect of MDSC, reduces MDSC levels, and blocks incision-induced mechanical hyperalgesia. OSU-53 can be used in studies related to breast cancer, prostate cancer, thyroid cancer, melanoma and postoperative pain .
Cat. No.: HY-170316
Ibetazol is a Importin β1 (KPNB1) inhibitor and nucleocytoplasmic transport disruptor. Ibetazol binds covalently to Cys585 of Importin β1, blocks both Importin β1-mediated direct transport and Importin α-dependent nuclear import processes, without affecting transport mediated by other nucleocytoplasmic transport proteins. Ibetazol induces cytoplasmic accumulation of Importin α1, and inhibits nuclear import of substrates carrying nuclear localization signals (NLS), including the NLS-cMyc reporter gene, RelA/p65 and SREBP1. Ibetazol triggers spindle malformation and chromosome misalignment by disrupting the mitotic function of Importin β1. Ibetazol inhibits the proliferation of cells expressing wild-type Importin β1. Ibetazol has a high activity-cytotoxicity window, lacks intrinsic fluorescence, and acts rapidly on nucleocytoplasmic transport processes. Ibetazol serves as a tool compound for investigating nuclear import processes specifically mediated by Importin β1 .
Cat. No.: HY-79602S
CAS No.: 1219795-34-2
Synonyms: p-Tosylamide-d4
Domaines de recherche:
4-Tolyl-d4-sulfonamide (p-Tosylamide-d4) is the d4-labeled p-Toluenesulfonamide (HY-79602). p-Toluenesulfonamide is a small-molecule anticancer agent and plasticizer. p-Toluenesulfonamide exerts antitumor activity by inducing lysosomal membrane permeabilization, cathepsin B release and lysosome-mediated cell death. p-Toluenesulfonamide modulates cholesterol distribution in lipid rafts of tumor cell membranes and the Akt/mTOR/p70S6K pathway. p-Toluenesulfonamide shows activity against various cancers including hepatocellular carcinoma, non-small cell lung cancer and tongue squamous cell carcinoma; intrapleural injection effectively reduces malignant pleural effusion without causing pleural adhesion. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T (HY-B0959) in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum. p-Toluenesulfonamide can be used in cancer-related research .
Cat. No.: HY-W007392
CAS No.: 934-05-4
Synonyms: Methyl 4-bromopyrrole-2-carboxylate
Cat. No.: HY-134096
CAS No.: 78323-98-5
Synonyms: DNS-M
Target:
Domaines de recherche:
Dansyl-morpholine (DNS-M) is a Fluorescent probe for lipid droplet imaging, cancer cell discrimination, and real-time tracking of lipid droplet dynamics. As a solvatochromic probe with a donor-π-acceptor structure, it relies on hydrophobic interaction for its mechanism of action: its good lipophilicity, confirmed by an oil-water partition coefficient LogP = 2.35, allows it to rapidly penetrate cell membranes, and it specifically localizes to the hydrophobic core of lipid droplets; its fluorescence is strongly enhanced in the nonpolar environment of lipid droplets, while it emits very weak fluorescence in polar environments like PBS buffer, and it exhibits a bathochromic shift in emission wavelength with increasing solvent polarity. It has negligible cytotoxicity, with cell viability remaining over 95% after 24-hour incubation with 100 μM of the probe, and it possesses excellent photostability, retaining over 97% of initial fluorescence intensity after 60 continuous laser scans. For cell imaging applications, its excitation/emission wavelengths for lipid droplet labeling are Ex/Em = 405/480−540 nm, and in a simulative lipid environment O/W emulsion, it has an excitation wavelength of ~346 nm and emission wavelength of ~500 nm, giving a Stokes shift of 154 nm[1].
Cat. No.: HY-171881
CAS No.: 864686-48-6
Domaines de recherche:
BI-5521 is an orally active GSK-3 inhibitor with an IC50 of 1.1 nM against GSK-3β. BI-5521 targets the two GSK-3 isoforms with similar potency and exhibits potent inhibitory activity against DYRK1A. By modulating GSK-3 activity, BI-5521 inhibits tumor proliferation and cancer cell growth, exerts cytotoxic effects, and reduces cancer cell viability. It shows consistent chemosensitivity across all subtypes of rhabdomyosarcoma, produces synergistic growth inhibitory effects when combined with SOS1 inhibitors, reduces oral glucose levels, regulates the myofibroblast differentiation pathway, decreases the nuclear localization of YAP/SMAD2/3, and lowers the positive rate of α-SMA in fibroblasts without affecting the apoptosis of CD4 + T cells. BI-5521 can be used in the research of non-small cell lung cancer, pleomorphic rhabdomyosarcoma, type 2 diabetes, pancreatic ductal adenocarcinoma, Alzheimer's disease, bipolar disorder, and metabolic dysfunction-associated steatotic liver disease .
Cat. No.: HY-109061A
CAS No.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
Cat. No.: HY-D3105
Target:
Domaines de recherche:
DCA is a Fluorescent probe for visualization of phase behavior in ER membranes. DCA is an ER-targeting, polarity-responsive NIR ratiometric probe, with its p-toluenesulfonamide group responsible for ER localization; its sensitivity to polarity relies on its donor-π-acceptor (D-π-A) structure, where aniline acts as the donor and dicyanomethylene acts as the acceptor, driving an intramolecular charge transfer (ICT) process upon excitation. In environments with low polarity, such as the closely packed, low water content ERₒ phase of ER membranes, DCA emits at a shorter wavelength, while in high polarity environments like the loosely packed, higher water content ERd phase, ICT leads to a red-shifted emission, allowing discrimination of the two phases via dual NIR emission colors and ratiometric imaging. Ex/Em = 488/570–620 nm and 488/665–735 nm; additional excitation/emission pairs include Ex/Em = 488/631 nm in low polarity 1,4-dioxane and Ex/Em = 488/677 nm in 1,4-dioxane with 30% water, the higher polarity condition. It shows a large Stokes shift of ~170 nm, and pH, viscosity, and biologically relevant species including Cys, GSH, H₂O₂, and metal ions do not exert marked interference on its fluorescence spectra[1].
Cat. No.: HY-P992056
Cat. No.: HY-W127487
CAS No.: 479050-96-9
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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
