SJ 172550

Names

[ CAS No. ]:
431979-47-4

[ Name ]:
SJ 172550

[Synonym ]:
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

Biological Activity

[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]:

Signaling Pathways >> Apoptosis >> MDM-2/p53

Research Areas >> Cancer

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ 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

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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