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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
20 Results for "
electrophile
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "electrophile" in MCE Product Catalog:
Research Areas:
Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
Target:
Research Areas:
PAD-IN-2 is a potent pad4 inhibitor (IC50: <1 μM). PAD-IN-2 can be used in the research of auto-immune diseases and cancers, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosis, cutaneous lupus erythematosis, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis and psoriasis .
Cat. No.: HY-D1336
CAS No.: 2183440-42-6
Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes .
Cat. No.: HY-W011134
CAS No.: 14464-31-4
Target:
Research Areas:
Palmitic acid N-hydroxysuccinimide is used to conjugate proteins to prepare targeted delivery vectors. Palmitic acid N-hydroxysuccinimide can be used as lipophilic electrophile. Palmitic acid N-hydroxysuccinimide can be used for the covalent connection between palmitic acid and ovalbumin. Palmitic acid N-hydroxysuccinimide can be used to synthesize cetacyl derivatives of amino acids, aminoacyl-trNA, coenzyme A, mercaptoacetic acid and other amino and thiogenic compounds .
Cat. No.: HY-130978
Research Areas:
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
Cat. No.: HY-19985A
CAS No.: 1858291-14-1
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
Target:
Research Areas:
BCP-T.A, a tunable heterocyclic electrophile, is a potent ferroptosis inducer by binding to GPX4 . BCP-T.A is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cat. No.: HY-W591393
CAS No.: 2669097-31-6
Cat. No.: HY-159591
CAS No.: 3060515-08-1
YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
Cat. No.: HY-D1376
CAS No.: 2183440-46-0
Cat. No.: HY-D1376A
CAS No.: 2183440-45-9
Cat. No.: HY-116879
CAS No.: 1680193-58-1
Synonyms: (2E)-4-Oxo-2-nonen-8-ynal; alkynyl-4-ONE
4-Oxo-2-Nonenal Alkyne ((2E)-4-Oxo-2-nonen-8-ynal; alkynyl-4-ONE) is a functionalized lipid electrophile that conjugated to the exosomes via the reaction of amino and aldehyde groups. 4-Oxo-2-Nonenal Alkyne can be used in tumor exosomes determination .
Cat. No.: HY-18408
CAS No.: 1415238-77-5
Synonyms: FAI
Target:
Research Areas:
5S rRNA modificator is a suitable electrophile for 2’-hydroxyl acylation on structured RNA molecules, yielding accurate structural information comparable to that obtained with existing probes; 5S rRNA RNA modification.
Cat. No.: HY-157919
CAS No.: 2377497-15-7
Synonyms: N-6-(Biotinylamino)hexanoyl-N'-[2-(N-maleimido)ethyl]piperazine, hydrochloride
Cat. No.: HY-163332
Research Areas:
MPO-IN-6 (compound ADC) is an electrophile with good antioxidant and anti-inflammatory properties. MPO-IN-6 is a myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD) inhibitor with IC50s of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 is a potential cardiovascular preventive agent .
Cat. No.: HY-L947
1,859 compounds
Built on druggable heterocyclic backbones with tunable electrophilic warheads (halogens, cyano groups), our electrophilic heterocyclic fragment library targets non-conserved cysteine/lysine residues and screens covalent ligands through an electrophile-first workflow. It generates high-quality dual-functional fragments for KRAS, BTK and other popular targets, supporting MS and DEL high-throughput screening to accelerate covalent drug lead discovery.
MCE Electrophilic Heterocyclic Fragment Library Built on druggable heterocyclic backbones with tunable electrophilic warheads (halogens, cyano groups), our electrophilic heterocyclic fragment library targets non-conserved cysteine/lysine residues and screens covalent ligands through an electrophile-first workflow. It generates high-quality dual-functional fragments for KRAS, BTK and other popular targets, supporting MS and DEL high-throughput screening to accelerate covalent drug lead discovery.
Cat. No.: HY-L913
105 compounds
Recently, significant advancements in tyrosine-targeting electrophiles have primarily occurred in the field of protein-protein interactions (PPIs), where cysteine residues are often underrepresented and novel chemistries are needed to address these interfaces. In this context, tyrosines are frequently more accessible compared to more buried binding sites. Moreover, they are commonly found at "hot spots," which are functional epitopes of PPIs, with 12.3% of the residues consisting of tyrosines. This prevalence is likely due to the hydrophobic nature of tyrosine, its ability to participate in aromatic π-interactions, and its capacity for hydrogen bonding. Beyond PPIs, some progress has also been made in covalent tyrosine targeting in other areas where more commonly addressed side chains are lacking. Even though tyrosine has a slightly lower pKa value compared to the protonated lysine side chain (approximately 10 vs. 10.5 for the unprotected amino acid side chains), significantly less progress has been made in the development of tyrosine-targeted covalent ligands compared to lysine. This is likely due to the reduced flexibility of the tyrosine side chain and the greater steric hindrance of its hydroxy group, which makes it more challenging to adopt suitable reaction geometries.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 124 fragment molecules which can target tyrosine residue and can be used for fragment-based covalent 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
