TAS4464

Overview

TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8 -activating enzyme ( NAE ) ( IC 50 =0.955 nM), and also inhibits CAII with an IC 50 of 0.73 μM, which is less potent than MLN4924 ( HY-70062 ). The IC 50 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.).

Application

Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Carbonic Anhydrase | Products > Signaling Pathways > NEDD8-activating Enzyme

Product Information

• Catalog No.: HY-128586
• CAS No.: 1848959-10-3
• Molecular Formula: C21H23FN6O6S
• Molecular Weight: 506.51
• Purity: 98.69%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
• Solubility: ≥ 2 mg/mL (3.95 mM); Clear solution
• Availability: In-stock

Source

Original product source