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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
29 Results for "
Structural modifications
" in MedChemExpress (MCE) Product Catalog:
Products (29)
29 Results for "Structural modifications" in MCE Product Catalog:
4
Category:
Natural Products Other disease Disease markers Endogenous metabolite Disease Research Fields Cancer
Target:
1
1 Cited Publications
Cat. No.: HY-P99033
CAS No.: 1905409-39-3
Synonyms: BTCT-4465A; RG-7828; RO7030816
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs). The Fc region of Mosunetuzumab incorporates a "knob-into-hole" structural modification and an N297G point mutation to achieve heterodimerization and eliminate Fc glycosylation, thereby effectively silencing antibody effector functions .
Cat. No.: HY-W087008
CAS No.: 6515-36-2
Cat. No.: HY-178099
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Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer .
Cat. No.: HY-147732
CAS No.: 2851838-08-7
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Intensive structural modification resulted in the identification of compound B15 as an effective sEH inhibitor with a value of 0.03 ± 0.01 nm, and the presence of soluble epoxide hydrolase (SEH) can reduce inflammation and pain.
Cat. No.: HY-18408
CAS No.: 1415238-77-5
Synonyms: FAI
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5S rRNA modificator is a suitable electrophile for 2’-hydroxyl acylation on structured RNA molecules, yielding accurate structural information comparable to that obtained with existing probes; 5S rRNA RNA modification.
Cat. No.: HY-118990
CAS No.: 246244-19-9
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Lobelane hydrochloride is a biologically active compound that has the activity of inhibiting vesicular monoamine transporter-2 (VMAT2). Lobelane hydrochloride has a low affinity for nicotinic acetylcholine receptors (nAChR), thereby enhancing its selectivity for VMAT2. Synthetic structural changes of lobelane hydrochloride have led to some related analogs that show mild changes in affinity for VMAT2. The most potent synthetic lobelane hydrochloride obtained after structural modification has a K(i) value of 630 nM, showing significant VMAT2 selectivity. The biological activity of lobelane hydrochloride suggests that it has the potential to be used in the development of compounds to inhibit methamphetamine abuse .
Cat. No.: HY-W114420
CAS No.: 17028-03-4
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3-Methyl-L-tyrosine is a derivative of L-Tyrosine (HY-N0473). Structurally, 3-Methyl-L-tyrosine features a methyl modification at the third position of the aromatic ring of L-Tyrosine. As a substrate for the protein tyrosine kinase Csk, 3-Methyl-L-tyrosine's relative catalytic efficiency (kcat/Km) is 38% of L-Tyrosine, indicating that the methyl modification impacts the processing efficiency of Gsk significantly. 3-Methyl-L-tyrosine helps to deepen the understanding of Gsk's molecular recognition mechanisms of its substrates, which is crucial for developing specific inhibitors targeting Gsk .
Cat. No.: HY-124209
CAS No.: 156406-33-6
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9-keto Fluprostenol is an analog of prostaglandin E2 (PGE2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. It is anticipated that this analog will have strong affinity for EP receptors and act as a PGE2 agonist.
Cat. No.: HY-123558
CAS No.: 74141-69-8
Synonyms: Y 14556
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Bactobolin C is an antibiotic produced by Pseudomonas sp. BMG13A7, which has strong antimicrobial and antitumor activities, can also inhibit antibody production and treat autoimmune encephalomyelitis. However, its undesirable toxicity limits its medicinal application. The unique chemical structure and promising biological activities of Bactobolin C have attracted people's interest in its total synthesis and new active analogs. So far, the structural modification of Bactobolin C has mainly focused on the hydroxyl groups on the amino acid side chains and backbone.
Cat. No.: HY-126911
CAS No.: 62145-07-7
Synonyms: Fluprostenol Prostaglandin D2
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11-keto Fluprostenol is an analog of prostaglandin D2 (PGD2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-11 of fluprostenol yields 11-keto fluprostenol. 11-keto Fluprostenol exhibits moderate binding to the CRTH2/DP2 receptor compared to PGD2 and essentially no activity at the DP1 receptor.
Cat. No.: HY-117063
CAS No.: 145204-80-4
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LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity .
Cat. No.: HY-180192
CAS No.: 3106089-54-4
Dehydroxy-oridonin-vinyl ester (Compound 6k) is an anti-cancer agent. Dehydroxy-oridonin-vinyl ester exhibits extremely strong anti-proliferative activity against SU-DHL-6 cells, with its IC₅₀ value being 0.12 μM. Dehydroxy-oridonin-vinyl ester induces cell apoptosis by inhibiting the activation of the PI3K/Akt signaling pathway, without affecting the cell cycle progression. Dehydroxy-oridonin-vinyl can be used for the study of lymphoma .
Cat. No.: HY-128230
CAS No.: 485362-61-6
Synonyms: MLS-0073383
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WAY-605337 (MLS-0073383) is a Bcl-B inhibitor, which can be used for structural modification and optimization of scaffolds .
Cat. No.: HY-184613
Polydopamine nanoparticles (PDA NPs) are nanoscale materials formed by the self-polymerization of dopamine monomers under specific conditions. Their structural characteristics include a polyphenolic structure and a surface rich in functional groups such as amino and phenolic hydroxyl groups, which provide abundant chemical modification sites.
Cat. No.: HY-L909
8,569 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged.
Covalent ligands rely on reactive groups (“warheads”), and new warheads are key to expanding the scope of covalent modalities. Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 8,900 fragment molecules with covalent modification potential, which can target various reactive amino acid residues and can be used for fragment-based covalent drug discovery.
Cat. No.: HY-L915
422 compounds
Lysine is the second most common target residue used in the design of TCIs and related covalent ligands. Its appeal lies in its abundance in human proteins, which is approximately three times higher than that of cysteine (5.8% vs. 1.9%). This significantly increases the number of proteins suitable for covalent targeting, especially given that many human proteins lack ligandable cysteine residues. Moreover, it has been suggested that functional lysines have a lower probability of being replaced by mutation, as they often play a crucial role in catalysis by acting as bases or nucleophiles. Additionally, lysines are essential for maintaining the structural integrity of proteins and for regulating post-translational modifications (PTMs). Consequently, targeting lysine has garnered significant interest in recent years.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 445 fragment molecules which can target lysine residue and can be used for fragment-based covalent drug discovery.
Cat. No.: HY-P11802
CAS No.: 126144-46-5
Cat. No.: HY-184608
CuS nanoparticles are nanomaterials with unique properties. Their structural characteristics endow them with excellent near-infrared light response, facilitating functional applications through surface modification. This material shows potential in the biomedical field, enabling synergistic photothermal and photodynamic therapies in tumor treatment, as well as precise drug delivery. In the energy sector, it is suitable for the development of novel energy storage devices; in the environmental field, it can participate in photocatalytic degradation processes.
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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
