444145

MDM2 Inhibitor

The MDM2 Inhibitor, also referenced under CAS 562823-84-1, controls the biological activity of MDM2.

• Synonym(s): MDM2 Inhibitor, trans-4-Iodo, 4ʹ-boranyl-chalcone, MDM2 Antagonist IV
• Empirical Formula (Hill Notation): C₁₅H₁₂BIO₃
• CAS Number: 562823-84-1
• Molecular Weight: 377.97
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale yellow
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C15H12BIO3/c17-14-8-1-11(2-9-14)3-10-15(18)12-4-6-13(7-5-12)16(19)20/h1-10,19-20H/b10-3+
• InChI key: BYMGWCQXSPGCMW-XCVCLJGOSA-N

Description

General description

A cell-permeable boranyl-chalcone compound that binds strongly to MDM2 and irreversibly disrupts MDM2/p53 protein complex formation. Exhibits selective toxicity to MDM2-overexpressing human breast cancer cell lines (IC₅₀ = 10 µM for MDA-MB-435, 8.8 µM for MDA-MB-231, and 7 µM for Wt-MCF7) compared to normal breast cell lines (IC₅₀ = 75 µM for MCF-10A and 63 µM for MCF-12A).

A cell-permeable boranyl-chalcone that binds strongly to MDM2 and irreversibly disrupts MDM2/p53 protein complex. Exhibits selective toxicity towards MDM2 overexpressing human breast cancer cell lines (IC₅₀ = 10, 8.8, and 7 µM for MDA-MB-435, MDA-MB-231, and Wt-MCF7, respectively) compared to normal breast cell lines (IC₅₀ = 75 and 63 µM for MCF-10A and MCF-12A, respectively).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MDM2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 10, 8.8, and 7 µM in selective toxicity for MDA-MB-435, MDA-MB-231, and Wt-MCF7, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kumar, S.K., et al. 2003. J. Med. Chem.46, 2813.

Legal Information

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Safety Information

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