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SJ 172550

MDMX inhibitor CAS# 431979-47-4

SJ 172550

Catalog No. BCC2416----Order now to get a substantial discount!

Product Name & Size Price Stock
SJ 172550: 5mg $92 In Stock
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Chemical structure

SJ 172550

3D structure

Chemical Properties of SJ 172550

Cas No. 431979-47-4 SDF Download SDF
PubChem ID 1317464 Appearance Powder
Formula C22H21ClN2O5 M.Wt 428.87
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 33.33 mg/mL (77.72 mM; Need ultrasonic)
Chemical Name methyl 2-[2-chloro-6-ethoxy-4-[(E)-(3-methyl-5-oxo-1-phenylpyrazol-4-ylidene)methyl]phenoxy]acetate
SMILES CCOC1=C(C(=CC(=C1)C=C2C(=NN(C2=O)C3=CC=CC=C3)C)Cl)OCC(=O)OC
Standard InChIKey RKKFQJXGAQWHBZ-LICLKQGHSA-N
Standard InChI InChI=1S/C22H21ClN2O5/c1-4-29-19-12-15(11-18(23)21(19)30-13-20(26)28-3)10-17-14(2)24-25(22(17)27)16-8-6-5-7-9-16/h5-12H,4,13H2,1-3H3/b17-10+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SJ 172550

DescriptionMDMX inhibitor. Reversibly binds MDMX (EC50 = 2.3 μM). Inhibits the MDMX-p53 interaction in cultured retinoblastoma cells; frees p53 to induce apoptosis.

SJ 172550 Dilution Calculator

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SJ 172550 Molarity Calculator

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Preparing Stock Solutions of SJ 172550

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3317 mL 11.6585 mL 23.3171 mL 46.6342 mL 58.2927 mL
5 mM 0.4663 mL 2.3317 mL 4.6634 mL 9.3268 mL 11.6585 mL
10 mM 0.2332 mL 1.1659 mL 2.3317 mL 4.6634 mL 5.8293 mL
50 mM 0.0466 mL 0.2332 mL 0.4663 mL 0.9327 mL 1.1659 mL
100 mM 0.0233 mL 0.1166 mL 0.2332 mL 0.4663 mL 0.5829 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on SJ 172550

MDMX inhibitor. Reversibly binds MDMX (EC50 = 2.3 μM). Inhibits the MDMX-p53 interaction in cultured retinoblastoma cells; frees p53 to induce apoptosis.

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References on SJ 172550

On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53.[Pubmed:22675482]

PLoS One. 2012;7(6):e37518.

SJ-172550 (1) was previously discovered in a biochemical high throughput screen for inhibitors of the interaction of MDMX and p53 and characterized as a reversible inhibitor (J. Biol. Chem. 2010; 285:10786). Further study of the biochemical mode of action of 1 has shown that it acts through a complicated mechanism in which the compound forms a covalent but reversible complex with MDMX and locks MDMX into a conformation that is unable to bind p53. The relative stability of this complex is influenced by many factors including the reducing potential of the media, the presence of aggregates, and other factors that influence the conformational stability of the protein. This complex mechanism of action hinders the further development of compound 1 as a selective MDMX inhibitor.

Identification and characterization of the first small molecule inhibitor of MDMX.[Pubmed:20080970]

J Biol Chem. 2010 Apr 2;285(14):10786-96.

The p53 pathway is disrupted in virtually every human tumor. In approximately 50% of human cancers, the p53 gene is mutated, and in the remaining cancers, the pathway is dysregulated by genetic lesions in other genes that modulate the p53 pathway. One common mechanism for inactivation of the p53 pathway in tumors that express wild-type p53 is increased expression of MDM2 or MDMX. MDM2 and MDMX bind p53 and inhibit its function by distinct nonredundant mechanisms. Small molecule inhibitors and small peptides have been developed that bind MDM2 in the p53-binding pocket and displace the p53 protein, leading to p53-mediated cell cycle exit and apoptosis. To date, peptide inhibitors of MDMX have been developed, but no small molecule inhibitors have been reported. We have developed biochemical and cell-based assays for high throughput screening of chemical libraries to identify MDMX inhibitors and identified the first MDMX inhibitor SJ-172550. This compound binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified. The effect of SJ-172550 is additive when combined with an MDM2 inhibitor. Results from a series of biochemical and structural modeling studies suggest that SJ-172550 binds the p53-binding pocket of MDMX, thereby displacing p53. This lead compound is a useful chemical scaffold for further optimization of MDMX inhibitors that may eventually be used to treat pediatric cancers and various adult tumors that overexpress MDMX or have similar genetic lesions. When combined with selective MDM2 inhibitors, SJ-172550 may also be useful for treating tumors that express wild-type p53.

Description

SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.

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