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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
19 Results for "
reactive cysteine residues
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "reactive cysteine residues" in MCE Product Catalog:
Synonyms: 5-TMRIA
Cat. No.: HY-177554
CAS No.: 2724919-69-9
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KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins .
Cat. No.: HY-D2381
Cat. No.: HY-130509
CAS No.: 81213-52-7
Synonyms: Otmpmms
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MTSSL (Otmpmms) is a highly reactive thiol-specific spin label that can be used to label thiol residues in proteins for the determination of protein structure and dynamics, as well as studies on protein-protein interactions. MTSSL serves as a nitroxide labeling reagent for cysteine residues in recombinant mouse prion protein (moPrP C) mutants. MTSSL can be applied in studies of transmissible spongiform encephalopathies (prion diseases) .
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CCW16 is a non-selective cysteine-reactive covalent ligand and an RNF4 E3 ubiquitin ligase recruiter with an IC50 of 1.8 μM against human RNF4[. CCW16 covalently modifies accessible cysteine residues on RNF4, PRDX1, PRDX2, and PRDX6, attenuating the peroxide-scavenging activity of peroxiredoxins. CCW16 induces oxidative stress through upregulation of HMOX1 and NRF2, and triggers ferroptosis via lipid peroxidation and ROS signaling pathways in an RNF4-independent manner. CCW16 serves as an RNF4-recruiting moiety; it does not induce RNF4 degradation when used alone and can be used to synthesize protein degraders, such as the PROTAC compound CCW 28-3 (HY-156774). CCW16 can be used for research on acute myeloid leukemia and hepatocellular carcinoma .
Cat. No.: HY-P4087
CAS No.: 1417221-06-7
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MTSEA hydrobromide is a sulfhydryl-reactive compound that modifies free cysteine residues to produce a positively charged side chain approximately the size of lysine .
Cat. No.: HY-D2002
CAS No.: 1219127-42-0
Cat. No.: HY-172721
CAS No.: 926905-86-4
Cat. No.: HY-W776833
CAS No.: 384342-58-9
Synonyms: Otmpmms-15N,d15
Cat. No.: HY-D1470
CAS No.: 210832-86-3
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BADAN is a thiol-reactive, environment-sensitive fluorescent probe used for site-specific labeling of protein cysteine residues to detect protein topology, local polarity, protein-lipid interactions, and conformational changes. The bromoacetyl group of BADAN covalently binds to cysteine thiols, and its fluorescence originates from the intramolecular charge transfer (ICT) excited state. The emission peak position varies with the polarity of the surrounding medium: it blue-shifts to approximately 488 nm in nonpolar environments (such as the hydrophobic core of lipid bilayers) and red-shifts to approximately 496-507 nm in polar environments (such as aqueous phases), independent of enzymes, pH, or membrane potential. Ex = 380-402 nm; Em = 400-600 nm .
Cat. No.: HY-P4087B
Cat. No.: HY-P10428
Cat. No.: HY-130509S
CAS No.: 1404308-02-6
Synonyms: Otmpmms-15N
Cat. No.: HY-D3579
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AF568 C5 Maleimide is a bright orange-red thiol-reactive fluorescent dye. AF568 C5 Maleimide selectively labels the thiol groups on cysteine residues in proteins, peptides and antibodies via stable thioether bonds (Ex/Em = 575/600 nm) .
Cat. No.: HY-W800719
CAS No.: 2665661-79-8
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N-Boc-N'-(PEG1-t-butyl ester)-L-Lysine-amido-Mal is the amino acid, lysine, with a maleimide at its C-terminus, a Boc-protecting group on its α-amine, and an amido-PEG1-t-butyl ester on its ε-amine. Maleimide is a thiol-reactive covalent group used to conjugate cysteine residues, while the Boc and the t-butyl ester can be later deprotected to perform further reactions.
Cat. No.: HY-L945
74 compounds
Sulfonyl fluoride (-SO₂F) overcomes the poor target selectivity of traditional covalent warheads that rely heavily on cysteine. With high stability and tunable electrophilicity under physiological conditions, it targets multiple nucleophilic residues including Lys, Tyr, Ser and His, offering expanded druggable space, lower off-target risks and prolonged efficacy. It is widely used in covalent inhibitors, molecular glues, PROTACs and chemical probes.
MCE has built a highly diverse sulfonyl fluoride fragment library with 1,162 structurally diverse, drug-like fragments. Designed for balanced reactivity, stability and compatibility, these molecules feature tunable electrophilicity, simple scaffolds and high derivatization potential. Combined with SuFEx click chemistry, the library enables efficient modular modification and rapid structure optimization.
Ideal for targeting non-cysteine residues, this library improves covalent screening and probe development efficiency, serving as a precise tool for early-stage covalent drug discovery and chemical biology research.
Cat. No.: HY-D3436
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Pt-Luc is a bioluminescent probe used for real-time, non-invasive monitoring of Pt (IV) prodrug reduction in living cells and animal models. The detection mechanism of Pt-Luc relies on the intracellular reduction mediated by active cysteine residues in proteins. Pt-Luc can penetrate the membrane of living cells; after entering cells, active cysteine thiolates in high-molecular-weight protein components reduce the Pt (IV) complex, thereby cleaving the caged aminoluciferin substrate. The released free aminoluciferin is then oxidized by luciferase in the presence of ATP to generate a bioluminescent signal, whose intensity is directly correlated with the reduction degree of Pt (IV) .
Cat. No.: HY-L908
1,244 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in 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
