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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
5779 Results for "
potential
" in MedChemExpress (MCE) Product Catalog:
Products (5779)
5779 Results for "potential" in MCE Product Catalog:
Cat. No.: HY-180185
Target:
Research Areas:
5-HT2A&5-HT2C agonist-2 (Compound 3ci) is a highly selective dual 5-HT2A/5-HT2C agonist that can cross the blood-brain barrier and has an EC50 < 1 μM. 5-HT2A&5-HT2C agonist-2 has high selectivity for 5-HT2B related to the risk of heart valve disease. 5-HT2A&5-HT2C agonist-2 can induce head convulsive responses, but has a relatively low hallucinogenic potential. 5-HT2A&5-HT2C agonist-2 can be used in the research of diseases such as depression and obesity .
Cat. No.: HY-183355
Research Areas:
KRAS G12D-IN-37 is a KRAS G12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRAS G12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRAS G12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer .
Cat. No.: HY-189215
CAS No.: 3087067-85-1
Target:
Influenza Virus RIG-I-like receptor (RLR) Toll-like Receptor (TLR) NF-κB Interleukin Related IFNAR Apoptosis Reactive Oxygen Species (ROS)
Research Areas:
Anti-Influenza agent 12 is an orally active inhibitor of influenza A virus infection. Anti-Influenza agent 12 inhibits RIG-I-mediated innate immune signaling and TLR3-mediated signaling pathways. Anti-Influenza agent 12 inhibits NF-κB phosphorylation and downregulates the expression levels of IRF3, ASC, iNOS, IL-4, IL-6, and IFN-α inflammatory genes. Anti-Influenza agent 12 inhibits viral nucleoprotein (NP) and matrix protein 2 (M2) mRNA transcription and protein synthesis. Anti-Influenza agent 12 inhibits virus-induced apoptosis, reduces ROS and NO production, and maintains mitochondrial membrane potential. Anti-Influenza agent 12 exhibits broad-spectrum activity against H1N1 and H3N2 subtypes, reduces viral load, and alleviates lung tissue damage. Anti-Influenza agent 12 can be used for research on influenza A virus infection .
Cat. No.: HY-189668
PI3K/AKT-IN-7 is a PI3K/Akt signaling pathway inhibitor with selective antiproliferative activity against hepatocellular carcinoma cells. PI3K/AKT-IN-7 downregulates the phosphorylation of PI3K and Akt and binds to NCF2 (Kd = 1.40 μM). PI3K/AKT-IN-7 induces apoptosis, S-phase cell cycle arrest, loss of mitochondrial membrane potential, and ROS accumulation, while inhibiting proliferation, migration, invasion, and DNA synthesis. PI3K/AKT-IN-7 inhibits tumor growth in a Hep3B xenograft BALB/c mouse model and reduces the expression of Ki67, PCNA, and MMP9. PI3K/AKT-IN-7 can be used for research on hepatocellular carcinoma .
Calcium propionate, meets analytical specification of E282 (Bioban-C, meets analytical specification of E282) is a calcium salt of Propionic acid with oral activity, which can be hydrolyzed into propionate and calcium ions. Calcium propionate, meets analytical specification of E282 elevates intracellular ROS levels in tumor cells, depletes GSH, reduces mitochondrial membrane potential, and thereby induces tumor cell apoptosis. In mouse colitis models, Calcium propionate, meets analytical specification of E282 modulates inflammatory factors such as IFN-γ, calprotectin, and Pglyrp3, ameliorating intestinal inflammation and metabolic disorders. In ruminants, Calcium propionate, meets analytical specification of E282 serves as a gluconeogenic precursor, regulating rumen fermentation and microbial diversity; in high-fat diet rats, it alters gut microbiota composition and affects blood biochemical parameters. Calcium propionate, meets analytical specification of E282 is commonly used as a food and feed additive, and is also used in research related to hypocalcemia, dyslipidemia, colitis, and lung cancer .
Cat. No.: HY-N16527
CAS No.: 233690-85-2
Synonyms: (-)-Cephaeline hydrochloride; NSC 32944 monohydrochloride
Cat. No.: HY-P4890
CAS No.: 1158181-62-4
Target:
RXFP Receptor Reactive Oxygen Species (ROS) Pyroptosis Caspase Interleukin Related TGF-beta/Smad AMPK Apoptosis
Research Areas:
Cat. No.: HY-W014589S
CAS No.: 1577233-55-6
Synonyms: 2,4-DTBP-d19
Cat. No.: HY-W749327
CAS No.: 1413431-25-0
Synonyms: 2,4-DTBP-d21
Cat. No.: HY-L154
3,728 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. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.
To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,728 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.
Cat. No.: HY-L941
4,236 compounds
Orthosteric sites are highly conserved, leading to poor subtype selectivity, off-target toxicity and drug resistance in traditional drugs. By contrast, allosteric sites show low conservation, high hydrophobicity, weak polarity, confined geometry and dynamic cryptic properties, granting modulators high selectivity, functional tunability and safety. Thus, allosteric therapy has become a major focus in drug discovery.
MCE curated nearly 1,000 clinical-stage allosteric modulators, analyzed PDB complex structures to identify key pharmacophores and privileged scaffolds, then designed and filtered compounds using rational “scaffold derivation + physicochemical screening” with strict property criteria. The resulting compounds show high rigidity and shape complementarity to shallow, dynamic, hydrophobic allosteric pockets.
This library comprises 4,315 diverse, lead-like compounds ideal for allosteric drug discovery and target screening, covering kinases, GPCRs and more. All are analogs of clinical-stage molecules with similarity > 0.6, combining high druggability and allosteric binding potential to support efficient early-stage R&D.
Cat. No.: HY-111297
CAS No.: 868843-84-9
Target:
Research Areas:
BMVC4 is a G-quadruplex (G4) stabilizer of the human telomeric sequence d[AG3(T2AG3)3]. Screening by circular dichroism (CD) spectroscopy revealed that BMVC4 is more suitable as the core molecule of G4 stabilizers than BMVC. The results showed that BMVC4-12C and BMVC4-8C3O are better candidates for G4 stabilizers and are worthy of further study. A simple and rapid screening method based on Cu2+-induced G4 unfolding can be used to find better G4 stabilizers for potential anticancer applications. CD results showed that the trivalent cations of 9-substituted BMVC derivatives are more suitable as G4 stabilizers than the divalent cations of BMVC. In addition, by monitoring the disappearance of the 291 nm CD band of human telomeres after Cu2+ addition, it was found that the core molecule of G4 stabilizer BMVC4 has better stability.
Cat. No.: HY-113720
CAS No.: 1041469-97-9
Target:
CDK Apoptosis Caspase Reactive Oxygen Species (ROS) JNK MDM-2/p53 Bcl-2 Family IGF-1R PI3K PKC Ras Akt
Research Areas:
RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G2/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer .
Cat. No.: HY-116161
CAS No.: 130273-87-9
Target:
Research Areas:
15(R)-17-phenyl trinor Prostaglandin F2α isopropyl ester (15(R)-17-phenyl trinor PGF2α isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (β) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2α isopropyl ester is a potential impurity in most commercial preparations of the latanoprost bulk drug product. The IC50 values for the free acid forms of 15(S)-17-phenyl trinor PGF2α and 15(R)-17-phenyl trinor PGF2α were determined to be 0.71 nM and 30 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle.1 A 3 μg dose of 15(R)-17-phenyl trinor PGF2α caused a 1.9 mmHg reduction of IOP in normotensive cynomolgus monkeys.
Cat. No.: HY-121337R
CAS No.: 61213-25-0
Synonyms: R-40244 (Standard)
Target:
Reference Standards Environmental Pollutants Apoptosis Bcl-2 Family Herbicide HSP PERK Eukaryotic Initiation Factor (eIF) Akt GSK-3 Reactive Oxygen Species (ROS)
Research Areas:
Flurochloridone (Standard) (R-40244 (Standard)) is the analytical standard of Flurochloridone (HY-121337). This product is intended for research and analytical applications. Flurochloridone (R-40244) is an orally active herbicide and an inducer of ER stress, apoptosis, and cytotoxicity. Flurochloridone upregulates GRP78 and activates the PERK-eIF2α-ATF4 UPR axis, ATF6, CHOP, Bax, and Bim. Flurochloridone decreases Akt, p-Akt, GSK3β, and p-GSK3β levels, and induces ROS, oxidative stress, γ-glutamyl cycle activation, and GSH accumulation. Flurochloridone inhibits mitochondrial respiration and ATP production while enhancing glycolysis and cell viability inhibition. Flurochloridone inhibits spermatogonial proliferation, spermatocyte meiosis, and sperm mitochondrial membrane potential, and induces Sertoli cell apoptosis and mitochondrial damage. Flurochloridone non-competitively binds phytoene desaturase, blocking phytoene desaturation and carotenoid synthesis, leading to leaf bleaching and phytotoxicity. Flurochloridone can be used for research on male reproductive toxicity, hepatotoxicity, and as a herbicide .
Cat. No.: HY-125740R
CAS No.: 7228-78-6
Synonyms: Malvidin-3-O-glucoside chloride (Standard); Oenin chloride (Standard)
Cat. No.: HY-177300
CAS No.: 1402802-45-2
Research Areas:
TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus .
Cat. No.: HY-18234AR
CAS No.: 103476-89-7
Category:
Calcium propionate, United States Pharmacopeia (USP) Reference Standard (Bioban-C (Pharmaceutical primary standard, USP)) is a calcium salt of Propionic acid with oral activity, which can be hydrolyzed into propionate and calcium ions. Calcium propionate, United States Pharmacopeia (USP) Reference Standard elevates intracellular ROS levels in tumor cells, depletes GSH, reduces mitochondrial membrane potential, and thereby induces tumor cell apoptosis. In mouse colitis models, Calcium propionate, United States Pharmacopeia (USP) Reference Standard modulates inflammatory factors such as IFN-γ, calprotectin, and Pglyrp3, ameliorating intestinal inflammation and metabolic disorders. In ruminants, Calcium propionate, United States Pharmacopeia (USP) Reference Standard serves as a gluconeogenic precursor, regulating rumen fermentation and microbial diversity; in high-fat diet rats, it alters gut microbiota composition and affects blood biochemical parameters. Calcium propionate, United States Pharmacopeia (USP) Reference Standard is commonly used as a food and feed additive, and is also used in research related to hypocalcemia, dyslipidemia, colitis, and lung cancer .
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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
