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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
1618 Results for "
Covalent
" in MedChemExpress (MCE) Product Catalog:
Products (1618)
1618 Results for "Covalent" in MCE Product Catalog:
Cat. No.: HY-P0112
CAS No.: 1027141-02-1
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Z-VAE (OMe)-FMK is a selective inhibitor of UCHL1, with better selectivity over UCHL3 and UCHL5. Z-VAE (OMe)-FMK binds to the active site cleft, covalently modifies the active site cysteine C90 to form a thioether bond, binds to inactive UCHL1 with a misaligned catalytic triad, and acts via a two-step addition-folding/migration/displacement mechanism. Z-VAE (OMe)-FMK stabilizes interactions through hydrogen bonding with oxyanion hole residues and van der Waals interactions with surrounding residues. Z-VAE (OMe)-FMK can be used in research related to colorectal cancer, lung cancer, pancreatic cancer, and Alzheimer's disease .
Cat. No.: HY-P10428
Cat. No.: HY-P10699
CAS No.: 487036-63-5
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Cat. No.: HY-P6299
CAS No.: 944792-75-0
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Cat. No.: HY-P990610
Cat. No.: HY-W097355
CAS No.: 5241-59-8
Synonyms: D-Phenylalanine amide; H-D-Phe-NH2
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(R)-2-Amino-3-phenylpropanamide (D-Phenylalanine amide) is a non-natural D-α-amino acid derivative and chiral amino acid amide. (R)-2-Amino-3-phenylpropanamide can be converted into D-Phenylalanine (HY-Y0079), which is applicable to the construction of all-D antimicrobial peptides and the synthesis of anti-HIV reagents. (R)-2-Amino-3-phenylpropanamide serves as a reagent for synthesizing benzoxaborole derivative 6, a dual covalent binder of Pseudomonas aeruginosa PBP3. (R)-2-Amino-3-phenylpropanamide is used in colon cancer-related research .
Cat. No.: HY-W591476
CAS No.: 134874-49-0
Synonyms: mPEG1000-SH
Cat. No.: HY-123048
CAS No.: 171744-39-1
Synonyms: PD022551; NSC 654077
DIBA-1 (PD022551; NSC 654077) is an inhibitor of HIV-1 nucleocapsid protein (NCp7). DIBA-1 displaces zinc from the zinc finger motifs of NCp7, p7NC and Pr55gag via thiol-disulfide exchange, covalently modifies cysteine residues, forms intermolecular disulfide cross-links, and disrupts zinc coordination. DIBA-1 inhibits zinc-dependent binding of NCp7 to HIV Ψ RNA, blocks the early replication process of HIV-1, suppresses the proteolytic processing of Gag precursors, and impairs the maturation and release of viral particles. DIBA-1 can be used in studies related to human immunodeficiency virus type 1 infection .
Cat. No.: HY-12455
CAS No.: 118292-34-5
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Duocarmycin A is an antitumor antibiotic and DNA alkylating agent with broad-spectrum antibacterial activity, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). Duocarmycin A selectively binds to the AT-rich minor groove of DNA, forms covalent adducts by alkylating the adenine N3 residue, thereby disrupting DNA structure and inhibiting its replication and transcription. Duocarmycin A induces apoptosis, sub-G1 phase accumulation and chromatin condensation, reduces the levels of pro-caspase-3/9, and induces p53-independent p21 expression. Duocarmycin A is widely used in the research of various malignancies, including leukemia, sarcoma, glioblastoma, as well as multiple solid tumor models such as lung cancer, breast cancer, and colorectal cancer .
Synonyms: N-Acetyl-L-serine
Cat. No.: HY-135146R
CAS No.: 2170136-65-7
Synonyms: (R)-GSK3482364 (Standard)
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GSK-3484862 (Standard) is the analytical standard of GSK-3484862 (HY-135146). This product is intended for research and analytical applications. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma .
Cat. No.: HY-13568R
CAS No.: 51234-28-7
Synonyms: LRCL 3794 (Standard)
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Benoxaprofen (Standard) is the analytical standard of Benoxaprofen. This product is intended for research and analytical applications. Benoxaprofen (LRCL 3794) is a nonsteroidal anti-inflammatory agent that blocks the biosynthesis of inflammatory mediators such as leukotrienes and prostaglandins by inhibiting 5-LOX, PGH2 synthase and cytochrome P-450. Benoxaprofen exhibits significant toxicity: it not only alters cellular redox status, uncouples oxidative phosphorylation and disrupts calcium ion homeostasis, but also causes liver injury through the formation of covalent adducts between its active metabolites and hepatic proteins. Benoxaprofen shows strong phototoxicity under ultraviolet irradiation, and induces erythrocyte lysis, mast cell degranulation and histamine release. Benoxaprofen is widely used in studies of urticaria and related phototoxic mechanisms .
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6-FAM-PEG3-Azide is a PEG-modified azide-functionalized fluorescein derivative that is used for labeling oligonucleotides. 6-FAM-PEG3-Azide is also a click chemistry reagent. It contains an Azide group and can undergo a copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing an Alkyne group. When 6-FAM-PEG3-Azide is co-incubated with boron clusters in a non-covalent manner, it enhances the cellular uptake and membrane permeability of 6-FAM (HY-66021). 6-FAM-PEG3-azide is applicable for fluorescence bioconjugation and probe development-related research .
Cat. No.: HY-145836
CAS No.: 2765240-52-4
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
Cat. No.: HY-146223A
Purity: 98.00%
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
Cat. No.: HY-147209
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DC-TEAD3in03 is a subtype-selective and covalent TEAD3 inhibitor with an IC50 of 0.16 μM. DC-TEAD3in03 exhibits the inhibitory activity on TEAD1/2/4 reduced by more than 100 times. DC-TEAD3in03 has the IC50 for TEAD3 of 1.15 μM in the GAL4-TEAD reporter gene experiment in cells, and it does not interfere with the β-catenin pathway. DC-TEAD3in03 reduces the growth rate of the zebrafish tail fin. DC-TEAD3in03 can be used to study the proportional growth of appendages in vertebrates .
Cat. No.: HY-14811
CAS No.: 251111-30-5
Synonyms: ZGN-440; CKD-732 free base
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Beloranib (ZGN-440; CKD-732 free base) is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib can be used in research on obesity and hypothalamic obesity .
Cat. No.: HY-148776
Cat. No.: HY-149465
CAS No.: 2298391-60-1
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STF-1623 is a highly potent, selective, cell-impermeable non-covalent ENPP1 inhibitor, with IC50 values of 0.6 nM and 800 nM against human ENPP1 and ENPP3, respectively. STF-1623 inhibits the hydrolysis of extracellular cGAMP by ENPP1, elevates intratumoral cGAMP levels, and indirectly enhances local cGAS-STING signaling and anti-tumor immunity in tumors. STF-1623 exhibits target-dependent retention in ENPP1-highly expressing tumors, while it undergoes rapid clearance in systemic circulation, and can penetrate into the CSF and brain parenchyma. STF-1623 can be used in studies related to breast cancer, pancreatic cancer, colorectal cancer, glioblastoma, and tumor immunology .
Cat. No.: HY-149933
CAS No.: 871978-21-1
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AM841 is a cannabinoid superagonist and a covalent, irreversible full agonist of CB1. AM841 can activate peripheral CB1 receptors to reduce excitatory neurotransmission and GI smooth muscle contractility, and inhibit synaptic transmission. AM841 is peripherally restricted at low doses in mice, with extremely low brain penetration, potently inhibits gastrointestinal motility, and can reverse acute stress-induced hyperaccelerated gastrointestinal transit; at high doses, it can produce the classic tetrad of central cannabinoid phenotypes (analgesia, catalepsy, hypothermia, decreased spontaneous activity). AM841 can improve intestinal inflammation in mouse colitis models. AM841 induces transient stress-induced hyperthermia. AM841 can be used for research on gastrointestinal motility disorders and colitis .
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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
