Molecular structure of SJ 172550, CAS Number: 431979-47-4
SJ 172550 (CAS 431979-47-4)
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Alternate Names:
2-[2-Chloro-4-[(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]-acetic acid methyl ester
Application:
SJ 172550 is a MDMX inhibitor that inhibits MDMX-p53 interaction in cultured cells
CAS Number:
431979-47-4
Purity:
≥95%
Molecular Weight:
428.87
Molecular Formula:
C22H21ClN2O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
SJ 172550, or MDMX Inhibitor II, is a potent inhibitor of MDMX that effectively disrupts the interaction between MDMX and p53 peptide, with an EC50 value of 4.3 µM. SJ 172550 achieves its inhibitory effect by forming a reversible covalent cysteine adduct within the p53-binding domain of MDMX. This interaction locks MDMX into a conformation that hinders its ability to bind with p53. The inhibitory action of SJ 172550 has significant implications. It induces apoptosis, triggers an increase in the expression of p53 target genes, and ultimately leads to p53-dependent cell death in retinoblastoma cells.
SJ 172550 (CAS 431979-47-4) References
- Identification and characterization of the first small molecule inhibitor of MDMX. | Reed, D., et al. 2010. J Biol Chem. 285: 10786-96. PMID: 20080970
- On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. | Bista, M., et al. 2012. PLoS One. 7: e37518. PMID: 22675482
- Synthesis and cytotoxic properties of novel (E)-3-benzylidene-7-methoxychroman-4-one derivatives. | Noushini, S., et al. 2013. Daru. 21: 31. PMID: 23587260
- Novel simplified yeast-based assays of regulators of p53-MDMX interaction and p53 transcriptional activity. | Leão, M., et al. 2013. FEBS J. 280: 6498-507. PMID: 24119020
- Studying p53 family proteins in yeast: induction of autophagic cell death and modulation by interactors and small molecules. | Leão, M., et al. 2015. Exp Cell Res. 330: 164-77. PMID: 25265062
- A tryptophanol-derived oxazolopiperidone lactam is cytotoxic against tumors via inhibition of p53 interaction with murine double minute proteins. | Soares, J., et al. 2015. Pharmacol Res. 95-96: 42-52. PMID: 25814188
- Medicinal Chemistry Strategies to Disrupt the p53-MDM2/MDMX Interaction. | Lemos, A., et al. 2016. Med Res Rev. 36: 789-844. PMID: 27302609
- Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors. | Stefaniak, J., et al. 2018. ACS Chem Biol. 13: 2849-2854. PMID: 30216042
Inhibitor of:
MDMX, SATB1, and WDR82.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SJ 172550, 10 mg | sc-357403 | 10 mg | $175.00 | |||
SJ 172550, 50 mg | sc-357403A | 50 mg | $737.00 |