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Merck

100081

14-3-3 Antagonist I, 2-5

The 14-3-3 Antagonist I, 2-5 controls the biological activity of 14-3-3.

Synonym(s):

14-3-3 Antagonist I, 2-5, (S)-2-(2-(4-Azidobenzamido)acetamido)-3-((4-hydroxyphenethyl)amino)-3-oxopropyl-dihydrogen phosphate

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About This Item

Empirical Formula (Hill Notation):
C20H23N6O8P
Molecular Weight:
506.41
UNSPSC Code:
12352200
Assay:
≥90% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze
desiccated (hygroscopic)
protect from light

Key Documents

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Product Name

14-3-3 Antagonist I, 2-5, The 14-3-3 Antagonist I, 2-5 controls the biological activity of 14-3-3.

assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

pale yellow to beige

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable dipeptidyl-phosphoserine compound that targets 14-3-3 phosphopeptide binding site and effectively competes against 14-3-3 ligands, including Raf-1 and p53, binding to 14-3-3 (IC50 = 2.6 µM against TMR-GG-RLSHpSSLPG binding to human 14-3-3ς). Shown to induce caspase-3 activation and apoptotic cell death in human lung adenocarcinoma A549 cultures (live cell population after 12 h 100 µM drug treatment = 30% of control). Stability study using A549 cell lysates (100 µM drug in 1 µg/ml lysate) reveals a dephosphorylation t1/2 of ~ 6 hrs and no detectable proteolytic degradation up to 12 hrs.

Other Notes

Wu, H., et al. 2010. Angew. Chem. Int. Ed.49, 6528.

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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