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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
271 Results for "
Enzyme Targets
" in MedChemExpress (MCE) Product Catalog:
Products (271)
271 Results for "Enzyme Targets" in MCE Product Catalog:
105
105 Publications Verification
Research Areas:
3-TYP is an inhibitor of SIRT3 (IC50of 38 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases .
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26 Cited Publications
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Bobcat339 is a potent and selective cytosine-based inhibitor of TET enzyme, with IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
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26 Cited Publications
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Bobcat339 hydrochloride is a potent and selective cytosine-based inhibitor of TET enzyme, with the IC50s of 33 μM and 73 μM for TET1 and TET2, respectively. Bobcat339 hydrochloride is useful to the field of epigenetics and serves as a starting point for new therapeutics that target DNA methylation and gene transcription .
19
19 Cited Publications
Cat. No.: HY-N0279
CAS No.: 18956-16-6
Synonyms: Cardamomin; Alpinetin chalcone
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10 Cited Publications
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TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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10 Cited Publications
Research Areas:
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
8
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Sulfadiazine is an orally active sulfonamide antibiotic. Sulfadiazine competitively inhibits p-aminobenzoic acid in the folic-acid-metabolism cycle, inhibiting multiplication of most Gram-positive and many Gram-negative bacteria. Sulfadiazine persists in soil long-term, and exerts selective pressure for sulfonamide-resistant microbial populations. Sulfadiazine targets Toxoplasma gondii DHPS enzyme. Sulfadiazine can be used for the research of congenital toxoplasmosis and bacterial infection .
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Sulfadiazine sodium is an orally active sulfonamide antibiotic. Sulfadiazine sodium competitively inhibits p-aminobenzoic acid in the folic-acid-metabolism cycle, inhibiting multiplication of most Gram-positive and many Gram-negative bacteria. Sulfadiazine sodium persists in soil long-term, and exerts selective pressure for sulfonamide-resistant microbial populations. Sulfadiazine sodium targets Toxoplasma gondii DHPS enzyme. Sulfadiazine sodium can be used for the research of congenital toxoplasmosis and bacterial infection .
8
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Sulfadiazine 100 µg/mL in methanol is an orally active sulfonamide antibiotic. Sulfadiazine 100 µg/mL in methanol competitively inhibits p-aminobenzoic acid in the folic-acid-metabolism cycle, inhibiting multiplication of most Gram-positive and many Gram-negative bacteria. Sulfadiazine 100 µg/mL in methanol persists in soil long-term, and exerts selective pressure for sulfonamide-resistant microbial populations. Sulfadiazine 100 µg/mL in methanol targets Toxoplasma gondii DHPS enzyme. Sulfadiazine 100 µg/mL in methanol can be used for the research of congenital toxoplasmosis and bacterial infection .
7
Category:
Microorganisms Antibiotics Resistance Selection Disease Research Antibacterial Other Antibiotics
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7 Cited Publications
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GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
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Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer .
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Microorganisms Antibiotics Animal Husbandry Disease Research Antibacterial Disease Research Fields Other Antibiotics Cancer
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Apramycin (Nebramycin II) is an orally active, acidic pH tolerant and aminoglycoside-modifying-enzymes-tolerant aminoglycoside antibiotic which inhibits protein biosynthesis by targeting the bacterial ribosome. Apramycin is a potential anti-drug-resistance antibiotic .
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I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes.?I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST .
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4 Cited Publications
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BAY-805, a chemical probe, is a selective inhibitor of ubiquitin-specific protease USP21. BAY-805 has high selectivity for deubiquitinating enzyme (DUB) targets, kinases, proteases and other common target enzymes .
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4 Cited Publications
NAT is an initial hit of NAMPT activator with an EC50 of 5.7 μM and a KD of 379 nM. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases .
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Category:
Flavonoids Leguminosae Flavonones Phenols Polyphenols Plants Sophora flavescens Aiton Disease Research Fields Cancer
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Apocynaceae Flavonols Flavonoids Other Diseases Phenols Polyphenols Plants Apocynum venetum Linn. Disease Research Fields
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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
