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NSC-144303

Cat. No. M5298
NSC-144303 Structure
Synonym:

Ubiquitin Isopeptidase Inhibitor I, G5

Size Price Availability
5mg USD 85  USD85 4-7 Days
10mg USD 145  USD145 4-7 Days
25mg USD 320  USD320 4-7 Days
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Quality Control & Documentation
Biological Activity

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


Protocol (for reference only)
Cell Experiment
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
Animal models
Formulation
Dosages
Administration
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Aleo E, et al. Cancer Res. Identification of new compounds that trigger apoptosome-independent caspase activation and apoptosis.

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Keywords: NSC-144303, Ubiquitin Isopeptidase Inhibitor I, G5 supplier, Apoptosis, inhibitors, activators


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