In vitro: G5 is capable of activating an apoptosome-independent apoptotic pathway. It targets the ubiquitinproteasome system by inhibiting the ubiquitin isopeptidases. G5 induces a rather unique apoptotic pathway, which includes 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. G5 is a potent apoptotic inducer showing IC50s of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.*The compound is unstable in solutions, freshly prepared is recommended
Cell Experiment | |
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Cell lines | IMR90-E1A (E1A) and E1A/C9DN cells |
Preparation method | Western blot of E1A cell lysates treated with stealth RNAi oligos specific for Apaf-1 or HDAC4 as indicated. E1A cells transfected with Apaf-1 or HDAC4-specific RNAi oligos were incubated for 20 hours with the indicated apoptotic insults. |
Concentrations | 1.25 μmol/L |
Incubation time | 20 h |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 414.39 |
Formula | C19H14N2O7S |
CAS Number | 108477-18-5 |
Form | Solid |
Solubility (25°C) | 10mM in DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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