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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
51 Results for "
covalent adducts
" in MedChemExpress (MCE) Product Catalog:
Products (51)
51 Results for "covalent adducts" in MCE Product Catalog:
18
2
2 Cited Publications
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CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
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1 Cited Publications
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CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450 .
Cat. No.: HY-164899
CAS No.: 2765091-45-8
Synonyms: 2-aminopyridine-3-carboxylic acid imidazolide
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2A3 (2-aminopyridine-3-carboxylic acid imidazolide) is a covalent probe reagent for Selective 2'-Hydroxyl Acylation analyzed by Primer Extension (SHAPE) that targets the RNA ribose 2'-OH group. 2A3 efficiently permeates the biological membranes of Gram-negative bacteria, Gram-positive bacteria, and mammalian cells. 2A3 exhibits no base bias and specifically labels conformationally flexible, unpaired regions within RNA.
2A3 forms covalent adducts by acylating the 2'-OH groups of flexible RNA residues. When combined with SHAPE-MaP (mutational profiling) sequencing technology, these modification sites are converted into detectable mutational signals, thereby accurately reflecting local RNA backbone flexibility and base-pairing status. 2A3 is primarily utilized in molecular biology and transcriptomics research, including the resolution of RNA structuromes in living cells, the study of RNA folding regulatory mechanisms, and the investigation of non-coding RNA functions .
Synonyms: LRCL 3794
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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 .
Cat. No.: HY-B0306
CAS No.: 14222-60-7
Synonyms: Protionamide
Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
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Propanedial (Malondialdehyde) (13.88 mM in water) is one of the final products of lipid peroxidation. Propanedial causes protein inactivation, DNA damage and cross-linking by forming stable covalent adducts with biological macromolecules, which is the main mechanism for its cytotoxicity and genotoxicity.
Propanedial production increases with the elevation of free radicals.
Propanedial is a key biomarker for evaluating the level of cellular oxidative stress [1][2][3].
Cat. No.: HY-W089800
CAS No.: 18829-56-6
Synonyms: trans-2-Nonen-1-al
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trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Cat. No.: HY-172615
CAS No.: 3033019-04-1
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AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .
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INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 can be used for the research of myeloid leukemia .
Cat. No.: HY-P10940
CAS No.: 845727-63-1
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Nitracrine inhibits RNA synthesis and covalently, reversibly binds to DNA but also forms covalent adducts with DNA in vivo. Nitracrine, a 1-nitroacridine derivative, is a potent hypoxia-selective agent in vitro and antitumor agent. Nitracrine has cytotoxicity towards most cells .
Cat. No.: HY-171036
CAS No.: 252212-58-1
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GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC50 of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD +, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .
Cat. No.: HY-171213
CAS No.: 3109123-46-5
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NB-3 is a nicotinamide adenine dinucleotide (NAD) hydrolase SARM1 inhibitor. NB-3 intercepts NAD hydrolysis and undergoes covalent conjugation with the reaction product adenosine diphosphate ribose (ADPR). The resulting small-molecule ADPR adducts are highly potent and confer compelling neuroprotection in neurological injury .
Synonyms: ADX-629
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Acloproxalap (ADX-629) is an orally active reactive aldehyde species (RASP) inhibitor. Acloproxalap binds covalently to free aldehydes, sequesters reactive aldehyde species, malondialdehyde, acetaldehyde and preformed malondialdehyde-acetaldehyde adducts, and reduces elevated RASP levels. Acloproxalap decreases the formation of aldehyde adducts, reduces liver and serum triglyceride levels, hepatic fat accumulation, circulating anti-malondialdehyde-acetaldehyde adduct antibody levels, and inhibits the release of IL-6 and MCP-1. Acloproxalap improves cell viability of liver slices exposed to ethanol. Acloproxalap blocks ethanol-induced damage in animal models of alcoholic liver disease. Acloproxalap is applicable to research related to alcoholic liver disease, alcoholic fatty liver disease, non-alcoholic steatohepatitis, chronic cough, rheumatoid arthritis, ulcerative colitis and mild atopic asthma .
Cat. No.: HY-N10686
CAS No.: 61077-78-9
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Synonyms: 4-HNE-d3
Cat. No.: HY-107767
CAS No.: 81307-24-6
Synonyms: DC 81
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Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct .
Cat. No.: HY-126256A
Purity: 99.50%
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PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
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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
