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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
3555 Results for "
fluorogenic caspace-3 substrate
" in MedChemExpress (MCE) Product Catalog:
Products (3555)
3555 Results for "fluorogenic caspace-3 substrate" in MCE Product Catalog:
Cat. No.: HY-50896R
CAS No.: 183321-74-6
Synonyms: CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)
Research Areas:
Erlotinib Standard (CP-358774 Standard) is the analytical standard of Erlotinib (HY-50896). This product is intended for research and analytical applications. Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis [3] .
Cat. No.: HY-50896S
CAS No.: 1034651-23-4
Synonyms: CP-358774-d6; NSC 718781-d6; OSI-774-d6
Cat. No.: HY-50896S1
CAS No.: 1211107-68-4
Synonyms: CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
Cat. No.: HY-50896S2
CAS No.: 1130852-41-3
Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4
Cat. No.: HY-50896S3
CAS No.: 1266656-97-6
Synonyms: CP-358774-d8; NSC 718781-d8; OSI-774-d8
Cat. No.: HY-W013724S
Synonyms: IDP-15N4 dilithium; Inosine-5'-diphosphoric acid-15N4 disodium
Cat. No.: HY-W1143867
CAS No.: 2226-71-3
Research Areas:
4’-Phosphopantetheine is an orally active coenzyme A (CoA) precursor. 4’-Phosphopantetheine is membrane-permeable and acts as a CoA precursor, a prosthetic group, and a reactive oxygen species (ROS) inhibitor. 4’-Phosphopantetheine binds covalently to rat liver fatty acid synthase, modifies the conserved serine residue in the PKS/NRPS carrier protein domain, and serves as a substrate for CoA synthase and PPAT. 4’-Phosphopantetheine undergoes non-catalytic exchange on rat liver fatty acid synthase, with a faster turnover rate than that of the enzyme complex, and restores intracellular CoA levels in cells with impaired de novo biosynthesis. 4’-Phosphopantetheine rescues phenotypes induced by CoA deficiency, normalizes PKAN-related biomarkers, restores mitochondrial enzyme activity, and alleviates vascular endothelial damage. 4’-Phosphopantetheine shows biological stability in serum, acts as a prosthetic group and degradation product of ACP, and inhibits the formation of atherosclerotic plaques. 4’-Phosphopantetheine can be used in the research of brain iron accumulation neurodegenerative diseases, pantothenate kinase-associated neurodegeneration, CoASY protein-associated neurodegenerative diseases, coronary heart disease, and atherosclerosis [3] .
Cat. No.: HY-L204
582 compounds
Lactic acid metabolism is one of the key metabolic pathways within living organisms. It plays a crucial role not only in cellular energy conversion but is also closely related to a variety of physiological and pathological processes. The production and clearance of lactic acid are important indicators of cellular metabolic balance, and its abnormal regulation may lead to conditions such as lactic acidosis, muscle fatigue, and hereditary metabolic diseases. Moreover, lactic acid is closely related to the malignancy of tumors and is considered a biomarker for malignant tumors and poor prognosis. Lactic acid can serve as a metabolic substrate to support the metabolic needs of tumor cells under hypoxic conditions, and it can also cause acidification of the tumor microenvironment, suppress immune cell function to promote immune evasion, and induce drug resistance in tumor cells. Currently, targeting lactic acid-lactylation and its related metabolic pathways has become a new research avenue for cancer treatment. In-depth exploration of the molecular mechanisms of lactic acid metabolism can help in screening lead compounds that regulate the lactic acid metabolism.
MCE contains 582 small molecule compounds targeting enzymes involved in lactic acid metabolism. This library is of significant value for researching the role of lactate metabolism in the mechanisms of diseases.
Cat. No.: HY-109061A
CAS No.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia [3] .
Synonyms: 1-Palmitoyl-2-linoleoyl PE; (1-Palmitoyl, 2-linoleoyl)-phosphatidylethanolamine; (1-Palmitoyl, 2-linoleoyl)-phosphoethanolamine
1-Palmitoyl-2-linoleoyl-sn-glycero-3-PE (1-Palmitoyl-2-linoleoyl PE; (1-Palmitoyl, 2-linoleoyl)-phosphatidylethanolamine; (1-Palmitoyl, 2-linoleoyl)-phosphoethanolamine) is a phosphatidylethanolamine phospholipid with a palmitoyl chain at sn-1 and a linoleoyl chain at sn-2, and an oxidation-prone substrate. 1-Palmitoyl-2-linoleoyl-sn-glycero-3-PE undergoes glycation and subsequent oxidation via Fenton system, forming long-chain and short-chain products at C-7, C-8, C-9, C-12 of its sn-2 acyl chain and glycated polar head. 1-Palmitoyl-2-linoleoyl-sn-glycero-3-PE’s glycated form oxidizes more quickly than non-glycated phosphatidylethanolamines and contributes to increased oxidative stress modifications. 1-Palmitoyl-2-linoleoyl-sn-glycero-3-PE can be used for the research of drug delivery .
Synonyms: 18:1 Lyso-PS
Research Areas:
Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium (18:1 Lyso-PS) is a modified PS product generated following NADPH oxidase activation and Lyso-PS signal transduction. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium signals through macrophage G2A to enhance the phagocytic uptake of PS-dependent apoptotic (apoptosis) neutrophils and PS-exposed activated neutrophils. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium enhances macrophage phagocytic uptake of apoptotic cells, carboxylate-modified microspheres, and PS-exposed non-apoptotic activated neutrophils. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium serves as an acyl acceptor substrate for the lysophosphatidyltransferase At1g78690p to generate diacylphosphatidylserine. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium reduces the secretion of IL-8 and decreases the proportion of viable colon cancer cells. 1-Oleoyl-2-hydroxy-sn-glycero-3-phospho-L-serine sodium is applicable to studies on peritonitis and inflammatory bowel disease [3].
Cat. No.: HY-170524
CAS No.: 3052313-73-9
Research Areas:
TDI-015051 is a highly selective, orally active antiviral agent that targets the coronavirus NSP14 guanine-N7 methyltransferase. TDI-015051 binds to substrates in a non-competitive manner and forms a stable ternary complex, precisely blocking the capping and methylation processes of viral mRNA. TDI-015051 potently inhibits a variety of coronaviruses (including SARS-CoV-2 and MERS). By impairing viral replication and translation and inducing a moderate type I interferon-mediated immune response, it significantly reduces pulmonary viral load and exhibits a synergistic effect with Nirmatrelvir (HY-138687). In addition, TDI-015051 does not inhibit non-coronavirus methyltransferases, and the drug-resistant mutations it induces impair viral fitness, demonstrating excellent antiviral properties and safety. TDI-015051 can be used for research on COVID-19 and the replication mechanism of coronaviruses .The IC50 values of TDI-015051 against SARS-CoV-2, α-hCoV-NL63, α-hCoV-229E, β-hCoV-MERS are 0.15 nM, 1.7 nM, 2.6 nM and 3.6 nM, respectively, and the Ka value against SARS-CoV-2 is 0.061 nM .
Cat. No.: HY-W657887
CAS No.: 154866-92-9
Target:
Histone Methyltransferase GSK-3 Tau Protein Amyloid-β Glucocorticoid Receptor Androgen Receptor Adrenergic Receptor
Research Areas:
GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease .
Cat. No.: HY-L015
1,149 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.
MCE owns a unique collection of 1,149 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.
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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
