MX69 NEW
Price | $31 | $44 | $72 |
Package | 1mg | 2mg | 5mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: MX69 | CAS No.: 1005264-47-0 |
Purity: 99.57% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | MX69 |
Description | MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation. |
Cell Research | The cytotoxic effect of leads is determined using the WST assay. Briefly, cells cultured in 96-well microtiter plates are treated with different concentrations of leads for a 20-hr period. WST (25 mg/well) is then added and incubation continued for an additional 4 hr, after which the optical density is read with a microplate reader.(Only for Reference) |
In vitro | MX69 inhibits expression of both MDM2 and XIAP in a time- and dose-dependent manner. MX69 induces ubiquitination of endogenous MDM2 in cancer cells. Downregulation of MDM2 by MX69 is through induction of MDM2 self-ubiquitination and degradation. Half-life of MDM2 in control-treated EU-1 cells is greater than 90 min, whereas MX69 treatment decreases the MDM2 half-life to <30 min. In SK-N-SH cells with stably transfected either wild-type (WT)-MDM2 or mutant MDM2-C464A, Treatment with MX69 significantly inhibits expression and increased the turnover of WT-MDM2 but not MDM2-C464A. MX69 significantly enhances the p53 half-life in WT-MDM2 but not mutant MDM2-C464A-transfected SK-N-SH cells. p53 is stabilized and accumulates in MX69-treated cells. MX69-mediated inhibition of XIAP is MDM2 dependent. Treatment of MX69 activates caspases 3, 7, and 9 as well as the cleavage of the death substrate PARP. MX69 also exhibits a significant cytotoxic effect on both ALL and NB lines(cancer cell lines), particularly those lines with MDM2 overexpression and a WTp53 phenotype. MX69-induced cell death is indeed due to apoptosis. MX69-induced cell apoptosis and death are dependent on MDM2, p53, and XIAP expression. MX69 shows minimal inhibitory effect on normal human bone marrow in vitro[1]. |
In vivo | MX69 has significant apoptotic and anti-proliferative effects on MDM2-expressing cancer cells in vivo. MX69 is well tolerated in animals due to the fact that normal cells/tissues express little or no MDM2. No evidence of toxicity after treatment with MX69 at the 100 mg/kg dose. MDM2-specific agent MX69 should not activate either on-target (e.g., p53 induction) or off-target signaling pathways in normal cells. Thus, specific MDM2 inhibitors such as MX69 may be excellent candidates for targeted therapy of refractory cancers expressing high levels of MDM2[1]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 88 mg/mL (185.4 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 39 mg/mL (82.2 mM) |
Keywords | E1/E2/E3 Enzyme | inhibit | E3 ligating enzyme | MX-69 | Ubiquitin ligase | IAP | E1 activating enzyme | E2 conjugating enzyme | Ubiquitin conjugating enzyme | Inhibitor | MX 69 | MX69 | Ubiquitin activating enzyme | MDM-2/p53 |
Inhibitors Related | Milademetan | NSC697923 | XI-006 | PYZD-4409 | Nutlin-3 | NAcM-OPT | NSC232003 | Xevinapant | NAE-IN-M22 | Indole-3-carbinol | Idasanutlin | RITA |
Related Compound Libraries | Cuproptosis Compound Library | Bioactive Compound Library | Ubiquitination Compound Library | HIF-1 Signaling Pathway Compound Library | Autophagy Compound Library | Pyroptosis Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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