Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303)是凋亡不依赖的半胱天冬酶和细胞凋亡的激活剂，对E1A和E1A/C9DN细胞的IC50值分别为1.76和1.6 μM 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. At higher concentrations (5-10 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO. 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 . At higher concentrations (5-10 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO.
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G5
CAS number：108477-18-5 molecular formula：C19H14N2O7S
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| Chinese alias | 3,5-双[[(4-硝基苯基)亚甲基]-2,3,5,6-四氢-4H-硫代吡喃-4-酮-1,1-二氧化物 | ||
| English alias | 3,5-Bis[(4-nitrophenyl)methylene]-2,3,5,6-tetrahydro-4H-thiopyran-4-one-1,1-dioxide | 3,5-bis((4-Nitrophenyl)methylene)-1,1-dioxide | tetrahydro-4H-thiopyran-4-one | NSC-144303 | Ubiquitin Isopeptidase Inhibitor I | tetrahydro-3,5-bis[(4-nitrophenyl)methy | ||
| CAS number | 108477-18-5 | molecular formula | C19H14N2O7S |
| molecular weight | 414.4 g/mol | Exact mass | ≥98% |
| PSA | 151.000 Ų | logp | 2.600 |
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