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431979-47-4

431979-47-4 structure
431979-47-4 structure
  • Name: SJ 172550
  • Chemical Name: SJ-172550
  • CAS Number: 431979-47-4
  • Molecular Formula: C22H21ClN2O5
  • Molecular Weight: 428.87
  • Catalog: Signaling Pathways Apoptosis MDM-2/p53
  • Create Date: 2018-05-26 23:00:06
  • Modify Date: 2024-01-04 09:42:57
  • 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.

Name SJ-172550
Synonyms Methyl {2-chloro-6-ethoxy-4-[(Z)-(3-methyl-5-oxo-1-phenyl-1,5-dihydro-4H-pyrazol-4-ylidene)methyl]phenoxy}acetate
Acetic acid, 2-[2-chloro-4-[(Z)-(1,5-dihydro-3-methyl-5-oxo-1-phenyl-4H-pyrazol-4-ylidene)methyl]-6-ethoxyphenoxy]-, methyl ester
MFCD03142926
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.
Related Catalog
Target

IC50: 5 μM (MDMX)[1]

In Vitro The p53 pathway is disrupted in virtually every human tumor. SJ-172550 binds the p53-binding pocket of MDMX, thereby displacing p53. SJ-172550 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 nutlin-3a[1]. SJ-172550 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[2].
References

[1]. Reed D, et al. Identification and characterization of the first small molecule inhibitor of MDMX. J Biol Chem. 2010 Apr 2;285(14):10786-96.

[2]. Bista M, et al. On the mechanism of action of SJ-172550 in inhibiting the interaction of MDM4 and p53. PLoS One. 2012;7(6):e37518.

Density 1.3±0.1 g/cm3
Boiling Point 560.8±60.0 °C at 760 mmHg
Molecular Formula C22H21ClN2O5
Molecular Weight 428.87
Flash Point 293.0±32.9 °C
Exact Mass 428.113892
LogP 3.73
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.586
Storage condition Store at +4°C
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
Risk Phrases 22
RIDADR NONH for all modes of transport