4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Property

Melting point:

233.5-234.5 °C

Boiling point:

693.0±55.0 °C(Predicted)

Density 

1.541±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C,unstable in solution, ready to use.

solubility 

≤15mg/ml in DMSO;1mg/ml in dimethyl formamide

form 

crystalline solid

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide Chemical Properties,Usage,Production

Description

Ubiquitin isopeptidase inhibitor I induces caspase activation and apoptosis (IC₅₀ = ~1.7 μM) through a Bcl-2-dependent and apoptosome-independent mitochondrial pathway that selectively inhibits ubiquitin isopeptidase activity (IC₅₀ = ~30 μM). It has also been shown to induce necrosis in apoptosis-resistant DKO cells.

Uses

Ubiquitin Isopeptidase Inhibitor I, G5 is a cell-permeable cross-conjugated unsaturated dienone compound.

in vitro

ubiquitin isopeptidase inhibitor i targeted the ubiquitinproteasome system via inhibiting the ubiquitin isopeptidases. ubiquitin isopeptidase inhibitor i could induce a rather unique apoptotic pathway, including a bcl-2-dependent but apoptosome-independent mitochondrial pathway with upregulation of the bh3-only protein noxa, stabilization of the inhibitor of apoptosis antagonist smac, but also the involvement of the death receptor pathway. moreover, the treatment of ubiquitin isopeptidase inhibitor i to cell extracts obtained from e1a cells did not inhibit the proteolytic activity of the proteasome, whereas mg-132 potently inhibited the cleavage of the llvy-amc substrate. in addition, noxa induction by ubiquitin isopeptidase inhibitor i could be inhibited by the specific rnai oligos efficiently. when apoptosis was scored, it was found that down-regulation of noxa was able to inhibit but did not suppress apoptosis and caspase activation in response to ubiquitin isopeptidase inhibitor i treatment [1].

IC 50

~30 μm

storage

Store at -20°C

References

[1] e. aleo, c. j. henderson, a. fontanini, et al. identification of new compounds that trigger apoptosome-independent caspase activation and apoptosis. cancer research 66(18), 9235-9244 (2006).