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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
12 Results for "
Nedd8-activating E1
" in MedChemExpress (MCE) Product Catalog:
Products (12)
12 Results for "Nedd8-activating E1" in MCE Product Catalog:
10
10 Cited Publications
Research Areas:
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.) [1].
10
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.) [1].
Cat. No.: HY-156744
Purity: 98.87%
Target:
Research Areas:
DBr-1 is a potent BRD9 PROTAC degrader with a DC50 of 90 nM. DBr-1 mediates the ubiquitination and proteasomal degradation of BRD9 via the ubiquitin-proteasome pathway. DBr-1 is applicable to research related to renal cell carcinoma and synovial sarcoma .
Cat. No.: HY-177936
CAS No.: 951950-33-7
Target:
Research Areas:
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 [1].
Cat. No.: HY-P810390
Synonyms: DKFZp566J164, EC 6.3.2., hUba3, MGC22384, Nedd8 activating enzyme E1 catalytic subunit, Nedd8 activating enzyme E1C, Nedd8 activating enzyme hUba3, Nedd8-activating enzyme E1 catalytic subunit, Nedd8-activating enzyme E1C, uba3
Cat. No.: HY-P703601
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: UBA3; Nedd8-activating Enzyme E1 Subunit 2; Prev. UBE1C; Nedd8-activating Enzyme E1C; Nedd8-activating Enzyme E1 Catalytic Subunit; UBA3, Ubiquitin-activating Enzyme E1 Homolog; HUba3; Ubiquitin-Like Modifier activating Enzyme 3; NAE2; Ubiquitin-Like Modifier-activating Enzyme 3; Ubiquitin-activating Enzyme E1C (Homologous To Yeast UBA3); Ubiquitin-activating Enzyme E1C; Ubiquitin-activating Enzyme E1C (UBA3 Homolog, Yeast); Nedd8-activating Enzyme HUba3; Ubiquitin Like Modifier activating Enzyme 3; Ubiquitin-activating Enzyme 3; NAE1; Proto-Oncogene Protein 1; Prev. APPBP1; Nedd8-activating Enzyme E1 Subunit; APP-BP1; Alternative Protein NAE1; Ula-1; Protooncogene Protein 1; Amyloid Beta Precursor Protein-Binding Protein 1, 59 KDa; A-116A10.1; Amyloid Beta Precursor Protein Binding Protein 1, 59kDa; NEDFIH; Nedd8-activating Enzyme E1 Regulatory Subunit; HPP1; Amyloid Protein-Binding Protein 1; Nedd8 activating Enzyme E1 Subunit 1; Amyloid Beta Precursor Protein-Binding Protein 1, 59kD
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-163105
CAS No.: 3072778-26-5
Target:
Research Areas:
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization [1].
Cat. No.: HY-P702529
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: NAE1; Proto-Oncogene Protein 1; Prev. APPBP1; Nedd8-activating Enzyme E1 Subunit; APP-BP1; Alternative Protein NAE1; Ula-1; Protooncogene Protein 1; Amyloid Beta Precursor Protein-Binding Protein 1, 59 KDa; A-116A10.1; Amyloid Beta Precursor Protein Bindi
Species:
Human
Source:
E. coli
Cat. No.: HY-P82386A
Synonyms: Nedd8 activating enzyme E1 subunit 1; HPP1; ula-1; APPBP1; A-116A10.1
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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
