NEDD8-activating Enzyme

Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC₅₀ of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice.

Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC₅₀ of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice.

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.).

NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.

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.).

ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.

AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease (NAAA) (IC₅₀ = 30 nM). The effect of AM9053 on FAAH activity is limited (IC₅₀ > 100 nM). AM9053 inhibits the proliferation of colorectal cancer cells by activating the PPAR-α and TRPV1 dependent mechanisms and induces S-phase cell cycle arrest. AM9053 alleviates intestinal fibrosis by regulating macrophage activity and inhibiting the IL-23 signaling pathway. AM9053 leads to an increase in NAE levels, especially PEA and OEA. AM9053 can be used for the study of colorectal cancer and intestinal fibrosis.

NAE-IN-1 (compound X-10) is a potent NAE1 inhibitor. NAE-IN-1 induces apoptosis and cell cycle arrest at the G2/M phase. NAE-IN-1 increases ROS levels and prevents cell migration. NAE-IN-1 shows anti-proliferation activity.

ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active.

Pevonedistat (Standard) is the analytical standard of Pevonedistat. This product is intended for research and analytical applications. Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice.

ZM223 hydrochloride (Standard) is the analytical standard of ZM223 hydrochloride (HY-101790A). This product is intended for research and analytical applications. ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.

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.

Pevonedistat hydrochloride (Standard) is the analytical standard of Pevonedistat hydrochloride (HY-10484). This product is intended for research and analytical applications. Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC₅₀ of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice.