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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
94 Results for "
covalent ligand
" in MedChemExpress (MCE) Product Catalog:
Products (94)
94 Results for "covalent ligand" in MCE Product Catalog:
5
5 Cited Publications
Cat. No.: HY-D2270
CAS No.: 2764890-88-0
4
4 Cited Publications
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KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .
3
3 Cited Publications
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .
3
3 Cited Publications
Cat. No.: HY-K0225
MCE Carboxyl Magnetic beads (200 nm, 10 mg/mL) are characterized by superparamagnetism, fast magnetic response, abundant carboxyl functional groups, monodispersity, and submicron scale particle size. Biological ligands (proteins, peptides, oligonucleotides, drug molecules, etc.) can be covalently coupled to the surface of microspheres under the action of special chemical reagents (such as EDC).
2
2 Cited Publications
EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis .
1
1 Cited Publications
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MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .
1
1 Cited Publications
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BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
1
1 Cited Publications
Cat. No.: HY-W229874
CAS No.: 757192-67-9
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EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1. EN106 reduces oxidative stress and rescues high glucose-induced impaired angiogenesis in HUVECs .
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1 Cited Publications
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EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination .
Cat. No.: HY-151716
CAS No.: 1808119-16-5
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Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples .
Synonyms: N-Methylmorpholine N-Oxide; MMNO; 4-Methylmorpholine 4-oxide
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4-Methylmorpholine N-oxide (N-Methylmorpholine N-Oxide; MMNO; 4-Methylmorpholine 4-oxide) is an amine oxide ligand and ozonation reagent. 4-Methylmorpholine N-oxide forms coordination complexes with lanthanum (III) nitrate and yttrium (III) nitrate via its nitroso oxygen atom. The metal-ligand bonds are dominated by electrostatic interactions with a small covalent component. 4-Methylmorpholine N-oxide is applicable in ozonation reactions for the synthesis of methyl 9-oxononanoate .
Cat. No.: HY-P10709
CAS No.: 847058-45-1
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Cat. No.: HY-W145665
CAS No.: 9005-82-7
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EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM
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-176812
CAS No.: 3055321-14-4
VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer .
Cat. No.: HY-168992
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UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases .
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(S)-SKBG-1 is an inactive and covalent NONO ligand, used for assay control..
Cat. No.: HY-W441004
CAS No.: 144735-82-0
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DSPE-Thiol is a modified phospholipid containing a reactive thiol group (-SH), featuring two saturated stearoyl chains, and used mainly for liposome and nanoparticle bioconjugation. DSPE-Thiol helps attach targeting ligands, stabilize membranes, and form covalent bonds .
Cat. No.: HY-158008
CAS No.: 2946593-60-6
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .
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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
