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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
1443 Results for "
weak
" in MedChemExpress (MCE) Product Catalog:
Products (1443)
1443 Results for "weak" in MCE Product Catalog:
Cat. No.: HY-134096
CAS No.: 78323-98-5
Synonyms: DNS-M
Target:
Research Areas:
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-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer .
Cat. No.: HY-L949
1279 compounds
Spirocyclic compounds, with rigid 3D structures, high Fsp³ and strong conformational restriction, are highly privileged scaffolds in small-molecule drug screening. They overcome drawbacks of planar aromatic compounds such as poor solubility, high off-target risks and weak druggability. Their orthogonal bicyclic geometry fits well into protein pockets, improving target affinity, subtype selectivity, metabolic stability and membrane permeability, making them ideal for hit identification against kinases, GPCRs, PPIs and other targets.
Spirocyclic scaffolds have been widely applied in oncology, antivirals, hypertension and CNS diseases, leading to many approved drugs and clinical candidates. SAR studies show that spiro-atom chirality, ring size and heteroatom substitution dominate bioactivity and selectivity, with the scaffold mainly serving as a conformational anchor. Azaspirocycles, spirooxindoles and spirosteranes target GPCRs, kinases, MDM2-p53 and PPIs. Approved drugs including irbesartan, spironolactone and rolapitant confirm their druggability, while revumenib and SAR405838 show promise against undruggable targets.
The MCE Spirocyclic Druglike Library contains over 1,000 diverse, stereospecific molecules selected by Lipinski’s rules. It covers privileged cores such as azaspirocycles, oxaspirocycles and spirooxindoles. These molecules bear rich chiral centers and distinct 3D orientations, reducing non-specific binding and enhancing screening efficiency. Featuring novel scaffolds, the library offers a highly innovative starting point for drug discovery.
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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!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
