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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
239 Results for "
Covalent binding
" in MedChemExpress (MCE) Product Catalog:
Products (239)
239 Results for "Covalent binding" in MCE Product Catalog:
Synonyms: N-Acetyl-L-serine
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-187684
CAS No.: 3054389-11-3
Research Areas:
FR-027 is an orally active, blood-brain barrier permeable XPO1 inhibitor with an EC50 value of 54-69 nM in human cells. FR-027 covalently modifies Cys528 of XPO1 via nucleophilic aromatic substitution, maintaining the nuclear export signal binding groove of XPO1 in a closed conformation to block the nuclear export process, and inhibits XPO1 function without inducing its protein degradation. FR-027 promotes cancer cell apoptosis and inhibits the growth of hematological and solid tumor cells. FR-027 can be used in research related to acute lymphoblastic leukemia, ovarian cancer, glioblastoma, and primary central nervous system lymphoma .
Cat. No.: HY-P11306
CAS No.: 247068-92-4
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Cat. No.: HY-P11902
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Cat. No.: HY-W012572
CAS No.: 351-50-8
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D-Histidine is an anti-biofilm agent that targets bacterial quorum sensing systems (such as RhlI/RhlR pathway) and has antibacterial activity. D-Histidine works by non-covalently binding to bacterial regulatory factors or copper ion complexes, selectively inhibiting bacterial biofilm formation and motility. D-Histidine downregulates quorum sensing-related gene expression, reduces the synthesis of virulence factors (such as alginate and proteases), and interferes with bacterial membrane stability, inhibiting biofilm formation, promoting the disintegration of mature biofilms, and enhancing antibiotic sensitivity. D-Histidine is also an efficient catalyst for the salt-induced peptide formation (SIPF) reaction, which promotes the condensation of amino acids to form dipeptides (such as dialanine and dilysine) by forming a complex with copper ions (Cu 2+) .
Cat. No.: HY-W012572A
CAS No.: 328526-86-9
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Cat. No.: HY-W115727B
CAS No.: 9003-05-8
Synonyms: PAM,Anion,Mw 18 million
Cat. No.: HY-W020780
CAS No.: 724722-89-8
Synonyms: mPEG5000-Maleimide
Cat. No.: HY-L924
1,488 compounds
Boronic acid and boronic ester represent a relatively novel and promising chemical structure in drug design. Boronic acid exists in an sp²-hybridized state, possessing an empty p-orbital that can act as a Lewis acid to accept lone pairs from heteroatoms (O, N, or S). This Lewis acidity enables it to form reversible covalent bonds with amino acid residues such as lysine, serine, threonine, and histidine. Currently, five FDA-approved drugs containing boronic acid or boronic ester predominantly involve such covalent binding mechanisms in their interactions with target proteins. Furthermore, boronic acid can serve as a bioisostere for carboxylic acids, phosphates, and phenolic groups, utilized to improve pharmacokinetic properties and enhance drug efficacy.
To date, five boron-containing drugs have been approved by the FDA. The unique properties of boronic acids and boronic esters confer significant potential in drug design, with applications spanning cancer therapy (e.g., multiple myeloma), anti-infectives (e.g., fungal infections, tuberculosis), anti-inflammatory treatments (e.g., atopic dermatitis), antibacterial agents (e.g., carbapenem-resistant bacterial infections), and Reactive Oxygen Species (ROS)-responsive prodrugs, among others. The MCE Boronic Acid/Boronic Ester Fragment Library, which contains 1,488 compounds, serves as a valuable tool for the development of boron-containing drugs.
Cat. No.: HY-182902
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IHMT-15137 is a BMX inhibitor with an IC50 of 26.97 nM. IHMT-15137 covalently binds to BMX Cys496 within the ATP-binding pocket, inhibits BMX phosphorylation at Tyr566, and disrupts the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis. IHMT-15137 reduces E2F1 protein stability via decreased Ser332/337 phosphorylation, increased ubiquitination, and ubiquitin-proteasome pathway degradation. IHMT-15137 induces cell cycle arrest, apoptosis, DNA damage, and suppresses cell migration and invasion. IHMT-15137 can be used for the research of small cell lung cancer .
Cat. No.: HY-W004588
CAS No.: 72914-19-3
tBu2bpy is a bidentate nitrogen ligand that coordinates with Pt (II) and Pt (IV) to form functional complexes. The tBu2bpy Pt (II) bis-crown ether complex selectively recognizes Mg 2+ and Zn 2+; both ions significantly enhance the fluorescence of the complex and cause a blue shift of the absorption peak. Its six-coordinate Pt (IV) complex [Pt (X)2Me2 ( tBu2bpy)] inhibits the proliferation of tumor cells. tBu2bpy Pt (IV) complexes bind to DNA through multiple interactions including partial intercalation, groove binding, and electrostatic interaction, and can competitively displace ethidium bromide and covalently bind to purine nucleotides. tBu2bpy can be used in relevant research in fields such as organic synthesis .
Cat. No.: HY-159591
CAS No.: 3060515-08-1
YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
Cat. No.: HY-W012572R
CAS No.: 351-50-8
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Cat. No.: HY-W996116
CAS No.: 1933460-23-1
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
AZM198 is an orally active myeloperoxidase (MPO) inhibitor. AZM198 irreversibly inactivates MPO (IC50=0.015 μM) via covalent binding to the heme prosthetic group, preferentially targets extracellular MPO activity, and reduces neutrophil extracellular trap formation, reactive oxygen species production and degranulation. AZM198 increases the fibrous cap thickness of atherosclerotic plaques, reduces lesion area, ameliorates hepatic steatosis and fibrosis in non-alcoholic steatohepatitis, and alleviates proteinuria and inflammatory infiltration associated with glomerulonephritis. AZM198 also decreases circulating levels of high-sensitivity Cardiac Troponin I and IL-1β, and mitigates endothelial cell injury. Therefore, AZM198 is suitable for research on various MPO-related diseases, including atherosclerotic cardiovascular disease, myocardial infarction, ischemic stroke, non-alcoholic steatohepatitis and crescentic glomerulonephritis .
Cat. No.: HY-149359
CAS No.: 3049485-80-2
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IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
Cat. No.: HY-D3072
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P6-Aggrate is a fluorescent probe for aggregated proteome detection. P6-Aggrate specifically recognizes amorphous aggregated proteomes through non-covalent reversible binding, and its fluorescence enhances after heat-induced protein aggregation. P6-Aggrate reflects the polarity and compactness heterogeneity within aggregated proteomes via emission wavelength shift: short-wavelength emission (blue shift) corresponds to large aggregates with high compactness, while long-wavelength emission (red shift) corresponds to small spots with low compactness (Ex/Em = 488/520-580 nm). P6-Aggrate enables reversible monitoring of the dynamic processes of formation and clearance of stress-induced proteome aggregation such as that induced by MG132 (HY-13259) in living cells. P6-Aggrate can be used in studies related to protein homeostasis imbalance, neurodegenerative diseases and protein aggregation .
Cat. No.: HY-163144
CAS No.: 3044084-97-8
DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia .
Cat. No.: HY-155882
CAS No.: 80506-64-5
Synonyms: mPEG750-NH2
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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
