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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
5225 Results for "
degrade
" in MedChemExpress (MCE) Product Catalog:
Products (5225)
5225 Results for "degrade" in MCE Product Catalog:
Target:
PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK
Research Areas:
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC. RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
Cat. No.: HY-15651S
Synonyms: AZD9668-13C,d3
Cat. No.: HY-180966
CAS No.: 3057939-66-6
Gly-PEG3-BA is an EML4-ALK PROTAC degrader. Gly-PEG3-BA effectively reduces EML4-ALK with a DC50 value of 0.50 μM in H3122 (EML4-ALK) cells. Gly-PEG3-BA effectively reduces EGFR mutant (L858R/T790M) levels with a DC50 of 20.15 μM in H1975 (EGER-L858R/T790M) cells. Gly-PEG3-BA exerts potent antiproliferation activity in H3122 (EML4-ALK) and H1975 (EGER-L858R/T790M) cells with IC50s value of 0.84 and 20.74 μM. Gly-PEG3-BA can be used for non-small lung cancer research .
Cat. No.: HY-183764
Research Areas:
COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC50 of 6.30 μM against sheep-derived COX-2 and an IC50 of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis .
Cat. No.: HY-183805
Target:
Research Areas:
5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pKi 7.24, human FAAH pIC50 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease .
Cat. No.: HY-79602S
CAS No.: 1219795-34-2
Synonyms: p-Tosylamide-d4
Research Areas:
4-Tolyl-d4-sulfonamide (p-Tosylamide-d4) is the d4-labeled p-Toluenesulfonamide (HY-79602). p-Toluenesulfonamide is a small-molecule anticancer agent and plasticizer. p-Toluenesulfonamide exerts antitumor activity by inducing lysosomal membrane permeabilization, cathepsin B release and lysosome-mediated cell death. p-Toluenesulfonamide modulates cholesterol distribution in lipid rafts of tumor cell membranes and the Akt/mTOR/p70S6K pathway. p-Toluenesulfonamide shows activity against various cancers including hepatocellular carcinoma, non-small cell lung cancer and tongue squamous cell carcinoma; intrapleural injection effectively reduces malignant pleural effusion without causing pleural adhesion. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T (HY-B0959) in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum. p-Toluenesulfonamide can be used in cancer-related research .
Cat. No.: HY-B1829AR
CAS No.: 2392-39-4
Synonyms: Dexamethasone 21-phosphate disodium (Standard)
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium (Standard) is the analytical standard of Dexamethasone phosphate disodium (HY-B1829A). This product is intended for research and analytical applications. Dexamethasone phosphate (Dexamethasone 21-phosphate) disodium is a prodrug form of the glucocorticoid Dexamethasone (HY-14648). Dexamethasone phosphate disodium is produced by introducing a phosphate ester group at the 21-position of the Dexamethasone molecule, forming a salt with sodium ions, thereby significantly improving water solubility. Dexamethasone phosphate disodium inhibits LPS (HY-D1056)-induced degradation of IRAK-1 and IRAK-4, and blocks LPS-induced activation of TRAF6, p-TAK1 and p-JNK. Dexamethasone phosphate disodium inhibits the secretion of RANTES, TGF-β1 and NO, promotes the production of MIP-1α and IL-10, and blocks microglial migration. Dexamethasone phosphate disodium is almost completely converted to Dexamethasone in rat blood, and supports transdermal delivery via iontophoresis. Dexamethasone phosphate disodium can be used in research related to steroid-dependent ulcerative colitis, chemotherapy-induced vomiting, allergic asthma and acute colitis (inflammatory bowel disease).
Cat. No.: HY-N0565AG
CAS No.: 10592-13-9
Cat. No.: HY-N0565BR
CAS No.: 24390-14-5
Synonyms: Doxycycline hydrochloride hemiethanolate hemihydrate (Standard); WC2031 (Standard)
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline hyclate (Standard) is the analytical standard of Doxycycline hyclate (HY-N0565B). This product is intended for research and analytical applications. Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
Cat. No.: HY-N0565S1
Cat. No.: HY-N7435R
CAS No.: 54814-64-1
Synonyms: (±)-Massoia lactone (Standard)
Category:
Cat. No.: HY-P2632C
Target:
Research Areas:
Cat. No.: HY-13443S
Synonyms: Exenatide (Leu-13C6,15N) TFA
Exendin-4 (Leu- 13C6, 15N) TFA (Exenatide (Leu- 13C6, 15N) TFA) is the 13C, 15N-labeled Exendin-4 (HY-13443). Exendin‑4 (Exenatide) is an orally active, blood-brain barrier-permeable glucagon-like peptide-1 receptor (GLP‑1 receptor) agonist that resists degradation mediated by dipeptidyl peptidase IV. Exendin‑4 mediates multiple glucose-regulating effects, including stimulation of glucose-dependent insulin secretion, inhibition of glucagon production, increase in β-cell mass, delay of gastric emptying, reduction of food intake, improvement of peripheral insulin sensitivity, and restoration of normal islet structure. Exendin‑4 inhibits oxidative stress, alleviates inflammatory responses, and reduces neuronal apoptosis. Exendin‑4 reduces the aggregation level of mutant huntingtin, improves motor function, prolongs survival time, and regulates the expression levels of leptin and ghrelin. Exendin‑4 can be used in research related to type 2 diabetes, acute ischemic stroke, and Huntington's disease .
Cat. No.: HY-141439
CAS No.: 936475-62-6
Research Areas:
TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
Cat. No.: HY-182759
Research Areas:
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
Cat. No.: HY-P11242
Research Areas:
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 .
Cat. No.: HY-L214
227 compounds
Liposomes are spherical or multilayered spherical vesicles formed by the self-assembly of diacyl chain phospholipids (lipid bilayers) in aqueous solutions, which can be made from natural or synthetic phospholipids and exhibit good biocompatibility and low toxicity. They can serve as delivery carriers for various bioactive substances (such as drugs, proteins, nucleic acids, etc.) and are widely used in biomedical and chemical research. The main advantages of liposomes include 1) Protective effect: Their bilayer structure can protect encapsulated molecules from enzymatic degradation, oxidation, and other influences, extending stability and activity; 2) Active targeting: Surface modifications enable active targeting, enhancing the concentration of drugs or molecules in specific tissues or cells; 3) Customizability: The composition and structure of liposomes can be adjusted according to needs, such as altering phospholipid types or adding targeting ligands. These properties make liposomes highly valuable in developing novel drug delivery systems, serving as nucleic acid carriers for gene transfection, studying cellular uptake mechanisms and drug release kinetics, as well as developing functional food additives to improve the bioavailability of nutritional components.
MCE contains 227 liposome compounds, which is a good tool for drug delivery-related studies.
Cat. No.: HY-10032A
CAS No.: 1247874-19-6
Target:
PF-477736 (hydrochloride) is an ATP-competitive Chk1 inhibitor (Ki 0.49 nM) that also inhibits CK2A1, PKCA, and Akt1, and is a broad-spectrum kinase inhibitor .PF-477736 induces apoptosis via PARP cleavage, caspase-3/7 activation, caspase-independent death, BAX and PUMA upregulation, H2AX phosphorylation, DNA fragmentation, and Chk1 proteasomal degradation, while inhibiting proliferation and preventing mitotic entry .PF-477736 demonstrates selective synthetic lethality in LIMD1-deficient cells, efficacy in subcutaneous xenograft models of LIMD1-deficient tumors, and anti-proliferative activity against leukemia and lymphoma cell lines .PF-477736 induces DNA double-strand breaks and activates the ATM-p53-p21 axis, and sensitizes CHK1i-insensitive neuroblastoma cells to apoptosis with ATM or DNA-PK inhibitors .PF-477736 can be used for the research of non-small cell lung cancer, leukemia, lymphoma, and neuroblastoma .
Cat. No.: HY-103605R
CAS No.: 1835705-55-9
Synonyms: VH032-C6-PEG3-C4-Cl (Standard); VHL Ligand-Linker Conjugates 12 (Standard); E3 ligase Ligand-Linker Conjugates 8 (Standard)
Research Areas:
(S,R,S)-AHPC-C6-PEG3-C4-Cl (Standard) is the analytical standard of (S,R,S)-AHPC-C6-PEG3-C4-Cl (HY-103605). This product is intended for research and analytical applications. (S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
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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
