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Merck
CN

5.08774

Sigma-Aldrich

Apoptosis Activator VIII, TP421

Synonym(s):

Apoptosis Activator VIII, TP421, (2-(7-(Diethylamino)-4-methyl-2-oxo-2H-chromen-3-yl)ethyl)triphenylphosphonium Salt

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About This Item

Linear Formula:
C34H35NO2P+Br- · H2O
UNSPSC Code:
12352200
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Assay

≥98% (HPLC)

Quality Level

form

powder

potency

400 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

General description

A cell-permeable triphenylphosphonium compound that exhibits selective toxicity towards cancer cells and inhibits their proliferation (IC50 = 400, 500, 800 nM and 1.1. µM for HPAC, MIA PaCa-2, BxPC-3, and PANC-1 pancreatic cancer cells, respectively). Arrests cell cycle at G0/G1 phase of the cell cycle in a time- and dose-dependent manner. It accumulates in mitochondria and induces mitochondrial and cytosolic accumulation of reactive oxygen species. Induces apoptosis by activating caspase-8 and 7 and by lowering the levels of Bcl-2 and survivin in cancer cells. Reduces autophagy as evidenced by a reduction in beclin-1 and increase in LC3B-II and p62 levels (at ~20 µM). Also shown to diminish Src phosphorylation (Tyr416) correspondingly reduce in Ser576 and Tyr861 phosphorylation in focal adhesion kinase (FAK).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

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

Millard, M., et al. 2013. PLos One.5, e13131.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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