444145
MDM2 Inhibitor
The MDM2 Inhibitor, also referenced under CAS 562823-84-1, controls the biological activity of MDM2.
别名:
MDM2 Inhibitor, trans-4-Iodo, 4ʹ-boranyl-chalcone, MDM2 Antagonist IV
InChI key
BYMGWCQXSPGCMW-XCVCLJGOSA-N
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+
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
Quality Level
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
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)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Srinivas K Kumar et al.
Journal of medicinal chemistry, 46(14), 2813-2815 (2003-06-27)
A series of boronic-chalcone derivatives were synthesized and tested for antitumor activity against human breast cancer cell lines. The results show the boronic-chalcones are more toxic to breast cancer cells compared to normal breast cells than other known chalcones.
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