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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
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
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Quality Segment

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

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.

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

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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