| Identification | Back Directory | [Name]
4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide | [CAS]
108477-18-5 | [Synonyms]
NSC-144303
Ubiquitin Isopeptidase-IN-G5
Ubiquitin Isopeptidase Inhibitor I
Ubiquitin Isopeptidase Inhibitor I, G5
G5, Ubiquitin Isopeptidase Inhibitor I
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC144303)
4H-Thiopyran-4-one,tetrahydro-3,5-bis[(4-nitrophenyl)methylene]-1,1-dioxide | [Molecular Formula]
C19H14N2O7S | [MDL Number]
MFCD28138111 | [MOL File]
108477-18-5.mol | [Molecular Weight]
414.39 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [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,unstable in solution, ready to use. | [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). |
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Nextpeptide Inc
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Energy Chemical
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www.energy-chemical.com |
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Bide Pharmatech Ltd.
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InvivoChem
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