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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
74 Results for "
covalent modification
" in MedChemExpress (MCE) Product Catalog:
Products (74)
74 Results for "covalent modification" in MCE Product Catalog:
35
Category:
Infection Acanthaceae Simsia foetida (Cav.) S.F.Blake Terpenoids Diterpenoids Plants Disease Research Fields Inflammation/Immunology
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25
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Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle .
5
5 Cited Publications
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EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner .
4
4 Cited Publications
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IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor that exerts its activity through covalent modification of His315 with an IC50 value of 110 nM. IDH1 Inhibitor 2 can dose-dependently reduce the intracellular reduced glutamine metabolic flux, thereby affecting cellular metabolic homeostasis. IDH1 Inhibitor 2 can be used to study the role of IDH1 in cellular metabolic regulation and cancer development .
2
2 Cited Publications
CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC50 of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification .
1
1 Cited Publications
Cat. No.: HY-124700
CAS No.: 1966129-74-7
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LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8 + T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors .
1
1 Cited Publications
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DI-1859 is a DCN1 and cullin 3 inhibitor with a Ki of <1 nM against human DCN1. DI-1859 forms a covalent bond with Cys115 of DCN1, cleaves its dimethylamino group, disrupts the DCN1-UBC12 interaction, and selectively inhibits the neddylation modification of cullin 3 relative to other cullins. DI-1859 inactivates CRL3, promotes the accumulation of NRF2 and SLC7A11, upregulates the expression of HO-1 and NQO1, reduces reactive oxygen species (ROS) levels, enhances insulin signaling, promotes insulin secretion, activates RhoA, regulates the phosphorylation of AKT, without completely blocking the neddylation modification of cullin 3 or restoring the expression of IRS-1. DI-1859 can be used in the research of Acetaminophen (HY-66005)-induced hepatotoxicity, hyperglycemia, metabolic dysfunction-associated steatotic liver disease, insulin resistance, breast cancer and lung cancer .
1
1 Cited Publications
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Supercinnamaldehyde is a potent transient receptor potential ankyrin 1 (TRPA1) activator with an EC50 value of 0.8 μM. Supercinnamaldehyde activates TRPA1 ion channels through covalent modification of cysteines .
1
1 Cited Publications
Cat. No.: HY-148775B
Purity: ≥95.0%
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PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) is a biodegradable amphipathic polymeric nanocarrier of poly (lactic-co-glycolic acid)-block-poly (ethylene glycol) (PLGA-PEG-Mal) that allows covalent modification of functional molecules. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) modified with Angiopep-2 can cross the blood-brain barrier and exhibits targeting selectivity for glioblastoma cells. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) can capture tumor-derived protein antigens, and exerts immunomodulatory effects when conjugated with anti-OX40 antibody; when used in combination with A2-CL/Dbait nanoparticles and radiotherapy, it prolongs survival time and reduces tumor volume in glioblastoma mouse models. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) can be used for studies related to bacterial wound infections and glioblastoma .
Cat. No.: HY-Y1353
CAS No.: 24424-99-5
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Di-tert-butyl dicarbonate (tBOC) is a covalent modification agent for hydroxyl groups (-OH) on the chitosan molecular chain. Di-tert-butyl dicarbonate selectively modifies chitosan and stabilizes the material structure through hydrophobic encapsulation. Di-tert-butyl dicarbonate reacts with the -OH groups of chitosan to form a hydrophobic layer, and in conjunction with triethylamine (TEA), removes trifluoroacetic acid (TFA) salts produced during the electrospinning process, preserving the nanofiber structure and high porosity of the membrane, and improving the material's cytocompatibility and mineralization-promoting ability. Di-tert-butyl dicarbonate can be used in research in the field of guided bone regeneration (GBR) .
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 .
Cat. No.: HY-155882
CAS No.: 80506-64-5
Synonyms: mPEG750-NH2
ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
Synonyms: N-Acetyl-L-serine
Synonyms: PiB; 6-OH-BTA-1
Research Areas:
Pittsburgh Compound B (PiB) is a blood-brain barrier-permeable, specific Aβ deposition PET tracer that binds to Aβ(1-40) fibrils with a Ki value of 678.4 nM. Through click chemical modification (a clickable Pittsburgh Compound B derivative is prepared by introducing a PEG3 linker and an alkynyl group at the 6-hydroxy site of Pittsburgh Compound B, followed by covalent conjugation with azide-labeled fluorescent dyes or affinity tags via copper-catalyzed azide-alkyne cycloaddition (CuAAC)), Pittsburgh Compound B and its conjugates can be used for fluorescence imaging, ultrastructural studies, and enrichment and characterization of Aβ complexes. Pittsburgh Compound B is applicable to Alzheimer's disease research .
Cat. No.: HY-U00447
CAS No.: 38275-34-2
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PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
Cat. No.: HY-W093017
CAS No.: 626-61-9
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4-Chloropyridine is a NNMT (Nicotinamide N-methyltransferase) substrate and suicide inhibition-based protein labeling scaffold precursor.4-Chloropyridine undergoes NNMT-catalyzed pyridine nitrogen methylation to increase C4 electrophilicity, enabling aromatic nucleophilic substitution by NNMT cysteine C159 for covalent NNMT modification and inactivation.4-Chloropyridine can be used for the research of various cancers .
Cat. No.: HY-P10940
CAS No.: 845727-63-1
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Cat. No.: HY-148775A
CAS No.: 743423-15-6
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MPEG-PLGA (21500-26500) is a biodegradable amphipathic polymeric nanocarrier of poly (lactic-co-glycolic acid)-block-poly (ethylene glycol) (PLGA-PEG-Mal) that allows covalent modification of functional molecules. MPEG-PLGA (21500-26500) modified with Angiopep-2 can cross the blood-brain barrier and exhibits targeting selectivity for glioblastoma cells. MPEG-PLGA (21500-26500) can capture tumor-derived protein antigens, and exerts immunomodulatory effects when conjugated with anti-OX40 antibody; when used in combination with A2-CL/Dbait nanoparticles and radiotherapy, it prolongs survival time and reduces tumor volume in glioblastoma mouse models. MPEG-PLGA (21500-26500) can be used for studies related to bacterial wound infections and glioblastoma .
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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
