662125
Ubiquitin Isopeptidase Inhibitor I, G5
The Ubiquitin Isopeptidase Inhibitor I, G5, also referenced under CAS 108477-18-5, controls the biological activity of Ubiquitin Isopeptidase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
别名:
Ubiquitin Isopeptidase Inhibitor I, G5, 3,5-bis((4-Nitrophenyl)methylene)-1,1-dioxide, tetrahydro-4H-thiopyran-4-one, NSC-144303
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关于此项目
经验公式（希尔记法）:
C19H14N2O7S
化学文摘社编号:
分子量:
414.39
MDL number:
NACRES:
NA.54
UNSPSC Code:
12352200
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable cross-conjugated α,β-unsaturated dienone compound that induces caspase activation and apoptosis (IC50 = 1.76 and 1.6 µM in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC50 = ~ 30 µM). The cellular expression of Bax and Bak is essential for G5-activated apoptosis, while Bcl-2 appears to protect cells against the effect of G5. G5 is more potent than, but otherwise exhibits similar pharmacological effects as, Ubiquitin Isopeptidase Inhibitor II, F6 (Cat. No. 662126). At higher concentrations (5-10 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Ubiquitin isopeptidase activity
Ubiquitin isopeptidase activity
Product does not compete with ATP.
Reversible: no
Target IC50: ~ 30 µM against ubiquitin isopeptidase activity; 1.76 and 1.6 µM for the induction of caspase activation and apoptosis in E1A and E1A/C9DN cells, respectively
Packaging
Packaged under inert gas
Preparation Note
Unstable in DMSO; reconstitute just prior to use.
Other Notes
Fontanini, A., et al. 2009. J. Biol. Chem.284, 8369.
Aleo, E., et al. 2006. Cancer Res.66, 9235.
Aleo, E., et al. 2006. Cancer Res.66, 9235.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Mustafa Yalcinkaya et al.
Journal of lipid research, 65(4), 100534-100534 (2024-03-25)
The deposition of cholesterol-rich lipoproteins in the arterial wall triggers macrophage inflammatory responses, which promote atherosclerosis. The NLRP3 inflammasome aggravates atherosclerosis; however, cellular mechanisms connecting macrophage cholesterol accumulation to inflammasome activation are poorly understood. We investigated the mechanisms of NLRP3
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