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MX69

Catalog No. T3653 CAS 1005264-47-0

MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.

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MX69, CAS 1005264-47-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 387.00
100 mg	In stock	$ 576.00
500 mg	In stock	$ 1,260.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.78%

Purity: 97.27%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MX69 is the MDM2/XIAP inhibitor, blocking the MDM2 protein-XIAP RNA interaction, leading to MDM2 degradation.
Targets&IC50	MDM2:2.34 μM(Kd)
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].
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)

Molecular Weight	474.57
Formula	C27H26N2O4S
CAS No.	1005264-47-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 88 mg/mL (185.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 39 mg/mL (82.2 mM)

References and Literature

1. Gu L, et al. Cancer Cell. 2016, 30(4):623-636.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Compound Library Bioactive Compounds Library Max PPI Inhibitor Library Anti-Colorectal Cancer Compound Library Ferroptosis Compound Library Anti-Aging Compound Library Anti-Pancreatic Cancer Compound Library Autophagy Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MX69 1005264-47-0 Apoptosis Ubiquitination E1/E2/E3 Enzyme IAP Mdm2 inhibit E3 ligating enzyme MX-69 Ubiquitin ligase E1 activating enzyme E2 conjugating enzyme Ubiquitin conjugating enzyme Inhibitor MX 69 Ubiquitin activating enzyme MDM-2/p53 inhibitor

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