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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
59 Results for "
E1 enzyme
" in MedChemExpress (MCE) Product Catalog:
Products (59)
59 Results for "E1 enzyme" in MCE Product Catalog:
26
26 Publications Verification
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PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
17
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Azoxymethane (AOM) is a colon carcinogen which leads to the formation of DNA adducts. Azomethane is a procarcinogen that requires metabolic activation via cytochrome P450 (P450) enzymes (primarily CYP2E1) .
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10
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.) .
10
10 Cited Publications
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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.) .
4
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Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
4
4 Cited Publications
Cat. No.: HY-B0876A
CAS No.: 56010-88-9
Synonyms: 4-Methylpyrazole hydrochloride
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Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
2
2 Cited Publications
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N106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research .
2
2 Cited Publications
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COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro .
2
2 Cited Publications
Cat. No.: HY-P74485
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: UBA1; Ubiquitin Like Modifier Activating enzyme 1; A1S9T; UBE1; GXP1; Ubiquitin‑Like Modifier‑Activating enzyme 1; Ubiquitin‑Activating enzyme E1; CFAP124; UBE1X; POC20; Ubiquitin‑Activating enzyme E1 (A1S9T And BN75 Temperature Sensitivity Complementing)
Species:
Source:
1
ATG7-IN-3 (Compound 18) is a potent ATG7 inhibitor with an IC50 of 0.048 μM. ATG7-IN-3 inhibits Autophagy. ATG7-IN-3 inhibits the formation of LC3B puncta. ATG7-IN-3 can be used in the researches of glioma and colon cancer .
Category:
Other Monoterpenes Terpenoids Other Diseases Plants Umbelliferae Vernonia Schreb. Disease Research Fields
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Cat. No.: HY-B1351
CAS No.: 84082-34-8
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Bilberry Extract is a bilberry extract, and its components include: Anthocyanidins. Bilberry Extract has potential antioxidant activity and can regulate specific metabolic enzymes in the liver, such as cytochrome P450 (CYP) 2C11 and CYP2E1 involved in drug metabolism. .
Cat. No.: HY-177936
CAS No.: 951950-33-7
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NAE-IN-3 (compound 1) is a potent, selective and non-covalent competitive NEDD8-activating enzyme (NAE) inhibitor (IC50 = 0.8 μM). NAE-IN-3 inhibits NAE by blocking the ATP-binding domain. NAE-IN-3 exhibits selectivity over analogous E1 enzymes UAE and SAE. NAE-IN-3 can be used for cancer research .
Cat. No.: HY-146177
CAS No.: 2531281-25-9
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CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
Cat. No.: HY-W679138
CAS No.: 128-03-0
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N,N-dimethyldithiocarbamate potassium is a ubiquitin-activating enzyme E1 inhibitor. N,N-dimethyldithiocarbamate potassium inhibits the activation of E1 and reduces the level of activated ubiquitinated E1 (ub-E1). N,N-dimethyldithiocarbamate potassium increases intracellular copper levels, enhances oxidative stress, elevates protein carbonyl levels, and upregulates the expression of HO-1 . N,N-dimethyldithiocarbamate potassium is applicable to research related to Parkinson's disease .
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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
