444155

MDMX Antagonist, SJ-172550 - CAS 431979-47-4 - Calbiochem

The MDMX Antagonist, SJ-172550, also referenced under CAS 431979-47-4, controls the biological activity of MDMX.

• Synonym(s): MDMX Antagonist, SJ-172550 - CAS 431979-47-4 - Calbiochem, Methyl-2-(2-chloro-6-ethoxy-4-(E)-(3-methyl-5-oxo-1-phenyl-pyrazol-4-ylidene)methyl)phenoxy)acetate, MDMX Inhibitor II
• Empirical Formula (Hill Notation): C₂₂H₂₁ClN₂O₅
• CAS Number: 431979-47-4
• Molecular Weight: 428.87
• MDL number: MFCD03142926
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (NMR)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable phenyl-pyraz-olylidene compound that competes with p53-derived peptide (aa 15-29) binding to MDMX in cell-free binding assays (EC₅₀ = 2.3 µM) in a reversible manner and effectively disrupts cellular p53-MDMX interaction (IC₅₀<20 µM in C33A, HER, and Weri1 cultures), while exhibiting much weaker affinity toward MDM2 (EC₅₀ = 26 µM in p53 peptide competition assays). MDMX inhibition by 20 µM SJ-172550 and MDM2 inhibition by 5 µM Nutlin-3a (Cat. Nos. 444143 & 444151) are both shown to result in reduced proliferation and increased cellular caspase-3 in cultured cells, however, only MDM2, but not MDMX, inhibition results in a significant p53 protein level upregulation.

A cell-permeable phenyl-pyrazolylidene compound that competes with p53-derived peptide (aa 15-29) binding to MDMX in cell-free binding assays (EC₅₀ = 2.3 M) in a reversible manner and effectively disrupts cellular p53-MDMX interaction (IC₅₀<20 M in C33A, HER, and Weri1 cultures), while exhibiting much weaker affinity toward MDM2 (EC₅₀ = 26 M in p53 peptide competition assays). MDMX inhibition by 20 M SJ-172550 and MDM2 inhibition by 5 M Nutlin-3a are both shown to result in reduced proliferation and increased cellular caspase-3 in cultured cells, however, only MDM2, but not MDMX, inhibition results in a significant p53 protein level upregulation.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Reed, D., et al. 2010. J. Biol. Chem.285, 10786.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable