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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
280 Results for "
membrane-permeable
" in MedChemExpress (MCE) Product Catalog:
Products (280)
280 Results for "membrane-permeable" in MCE Product Catalog:
Cat. No.: HY-184325
NDM-622 is a Colistin (HY-113678) adjuvant. NDM-622 weakly inhibits IKKβ with an IC50 of 20.40 μM. NDM-622 reduces the minimum inhibitory concentration of colistin against colistin-highly-resistant Acinetobacter baumannii and Klebsiella pneumoniae. NDM-622 decreases bacterial colony-forming units in a mouse peritonitis model infected with colistin-highly-resistant Klebsiella pneumoniae. NDM-622 does not modify bacterial lipid A, induce reactive oxygen species production, or increase bacterial membrane permeability. NDM-622 can be used in the research of extensively drug-resistant Gram-negative bacterial infections, colistin-resistant Acinetobacter baumannii infections, and Klebsiella pneumoniae infections .
Cat. No.: HY-184980
CAS No.: 2180967-88-6
Urease-IN-23 is a cryptococcal urease inhibitor with antifungal activity. AF55 exhibits mixed-type inhibition against cryptococcal urease, binds to both the nickel ion site at the enzyme's catalytic center and the allosteric site, impairs urease catalytic efficiency, simultaneously disrupts fungal virulence structures and damages cell membrane integrity. The IC50 and Ki values of Urease-IN-23 against cryptococcal urease are 54.92 nM and 149.1 nM, respectively. Urease-IN-23 significantly reduces the capsule thickness of Cryptococcus neoformans and Cryptococcus gattii, increases fungal cell membrane permeability, and completely blocks melanin synthesis. Urease-IN-23 shows no toxicity in the Galleria mellonella larval model. Urease-IN-23 can be used in studies related to fungal infections .
Cat. No.: HY-187173
Target:
Research Areas:
CAXII-IN-4 is a human carbonic anhydrase XII (hCA XII) inhibitor with Ki values of 4.9, 3079, 62.5 and 58.4 nM against hCA XII, hCA I, hCA II and hCA IX, respectively, showing high selectivity toward tumor-associated hCA XII. CAXII-IN-4 binds to the active site of hCA XII via a classic sulfamide binding mode, coordinates with Zn 2+, forms a hydrogen bond with Ser133, and stabilizes the enzyme complex to reduce structural deviation. CAXII-IN-4 possesses both lipophilicity and polarity, and is predicted to have superior membrane permeability and oral absorbability. CAXII-IN-4 can be used in studies related to tumor-associated carbonic anhydrase inhibition .
Cat. No.: HY-D0920
CAS No.: 166196-17-4
Cat. No.: HY-D3573
Target:
Research Areas:
AF488 C5 Maleimide is a thiol-reactive Fluorescent dye used to label target proteins and bacterial structures. AF488 C5 Maleimide irreversibly forms covalent thioether conjugates with cysteine thiol groups. AF488 C5 Maleimide stabilizes pre-formed globular low-molecular-weight Tau protein oligomers by blocking cysteine-dependent tau protein aggregation, allowing observation of the internalization process of tau protein oligomers into neuronal cells via confocal microscopy. AF488 C5 Maleimide can label cysteine-modified pili; the outer membrane permeability varies among different bacterial species, allowing imaging via epifluorescence microscopy using a FITC filter set .
Cat. No.: HY-N6043
CAS No.: 69039-02-7
Cat. No.: HY-138008
CAS No.: 1415262-07-5
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WX-132-18B is a tubulin inhibitor with an IC50 of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer .
Cat. No.: HY-179038
CAS No.: 433702-41-1
PYO12 is a 3-phenyl-4-phenoxypyrazole type antibacterial compound. PYO12 exhibits selective activity against Gram-positive bacteria with MIC for S. aureus, B. subtilis, S. pneumoniae, and MRSA of 1, 1, 1, and 4 μg/mL respectively. PYO12 has no activity against Gram-negative bacteria. PYO12 can significantly increase bacterial membrane permeability and significantly upregulate cell wall stress-related genes, possibly by binding to the C55-PP part of lipid II. PYO12 shows a concentration-dependent bactericidal effect, has low toxicity to mammalian cells, and does not cause hemolysis. PYO12 can be used to develop new antibiotics targeting bacterial cell wall synthesis .
Cat. No.: HY-L144
1,112 compounds
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 mitochondrial membrane, the so-called mitochondrial membrane permeability transition (MMPT). MMPT is caused by the opening of pores in the inner mitochondrial membrane, 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 1,112 compounds with identified and potential mitochondrial protective activity. MCE Mitochondrial Protection Compound Library is critical for drug discovery and development.
Cat. No.: HY-173437
CW-2 is a CRBN-recruited PARP1 PROTAC degrader. CW-2 triggers multiple downstream biological effects including DNA damage accumulation, impaired DNA repair, mitochondrial-mediated apoptosis, intracellular ROS buildup and G1/S cell cycle arrest, as well as the regulation of oxidative phosphorylation, p53, PI3K-Akt and MAPK alongside ubiquitin proteolysis pathways. CW-2 enhances cell membrane permeability and intracellular platinum enrichment, exhibits detectable pharmacokinetic profiles after intraperitoneal administration in rats and drives differential gene expression. CW-2 can be applied to research on triple-negative breast cancer, non-small cell lung cancer, cisplatin-resistant non-small cell lung cancer, colon cancer and pancreatic cancer .
Cat. No.: HY-D1737
Cat. No.: HY-N0570S
CAS No.: 1330260-89-3
Synonyms: DOPET-d4; 3,4-Dihydroxyphenethyl alcohol-d4; 3-Hydroxytyrosol-d4
Cat. No.: HY-N0570S1
Synonyms: DOPET-d5; 3,4-Dihydroxyphenethyl alcohol-d5; 3-Hydroxytyrosol-d5
Cat. No.: HY-N6043R
CAS No.: 69039-02-7
Cat. No.: HY-D3401
CAS No.: 3121511-17-6
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LHA585 is a fluorescent probe targeting the lipid hydrogen abstraction process for the early detection of ferroptosis (Ferroptosis). Its detection mechanism relies on the reactivity of its own 4-phenyl-3-methylbut-2-enyl moiety with biologically relevant oxidative radicals, including peroxyl radicals (ROO·), alkoxyl radicals (RO·), hydroxyl radicals (HO·), and peroxynitrite anions (ONOO−); upon hydrogen abstraction from this structure, radical rearrangement and radical cleavage occur, releasing a xanthene radical which converts into a highly fluorescent rhodamine dye in biological environments, thereby achieving a fluorescence turn-on ratio of up to 360-fold. LHA585 is non-fluorescent in its native state, possesses excellent membrane permeability due to its non-polar property, and the rhodamine dye generated after oxidation diffuses into mitochondria. The excitation wavelength of LHA585 is 561 nm, and its emission wavelength ranges from 570 to 620 nm .
Cat. No.: HY-N0570R
CAS No.: 10597-60-1
Synonyms: DOPET (Standard); 3,4-Dihydroxyphenethyl alcohol (Standard); 3-Hydroxytyrosol (Standard)
Cat. No.: HY-D3127
CAS No.: 455251-97-5
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DCA-Mln is a Fluorescent probe for ferric iron (Fe³⁺) detection. The probe works via an internal charge transfer (ICT) process from its diethylamino group to its dicyano group, which produces bright pink fluorescence in its unbound state; when Fe³⁺ is present, two molecules of DCA-Mln chelate with one Fe³⁺ ion, with one cyano group of each DCA-Mln participating in the complexation, and this binding triggers a photoinduced electron transfer (PET) process that provides a nonradiative deactivation pathway, resulting in fluorescence quenching; additionally, the probe exhibits a visible color change from purple to peach pink upon Fe³⁺ binding, enabling dual-channel detection. The probe has an excitation wavelength of 570 nm and an emission wavelength of 670 nm, and it shows a rapid response, with fluorescence stabilizing within 15 seconds of Fe³⁺ addition. DCA-Mln is cell-membrane-permeable, nontoxic at the imaging concentration of 10 μM, and can be used for Fe³⁺ detection in actual water samples, Fe³⁺ imaging in living cells, and as an anti-counterfeiting ink[1].
Cat. No.: HY-N17617
CAS No.: 70238-51-6
Cat. No.: HY-D3128
CAS No.: 2348351-60-8
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Mito-RhFe is a Fluorescent probe for mitochondrial labile Fe³⁺ monitoring via imaging and flow cytometry. This probe is a rhodamine-based construct with a spirolactam fluorescence signaling group and an N2-hydroxyethyldiethylenetriamine chelator; its delocalized positive charge enables mitochondria-targeting ability in live cells, and it exhibits fine cell membrane permeability. In its native state, it exists in the non-fluorescent spirolactam form, but upon binding to Fe³⁺, it undergoes a ring-opening conversion to the fluorescent rhodamine form, triggering a turn-on fluorescent response; this process is reversible, as the addition of the metal chelator TPEN removes Fe³⁺ and converts the probe back to its non-fluorescent spirolactam form, and re-addition of Fe³⁺ restores fluorescence. The probe shows high selectivity for Fe³⁺ over most other metal cations present in living systems, with a ~90-fold fluorescence enhancement upon binding to 20 equiv of Fe³⁺. Mito-RhFe has excitation/emission wavelengths of Ex/Em = 540/578 nm, with an ~8 nm bathochromic shift in emission upon Fe³⁺ binding, and it can also be excited at 543 nm for confocal imaging with emission detected at 570-620 nm[1].
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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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
