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GSK2643943A

Cat. No. M9871
GSK2643943A Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 165  USD165 In stock
25mg USD 330  USD330 In stock
50mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor targeting USP20/Ub-Rho with an IC50 of 160 nM.

Chemical Information
Molecular Weight 277.3
Formula C17H12FN3
Solubility (25°C) DMSO 90 mg/mL
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] Jeanine A Harrigan, et al. Nat Rev Drυg Discov. Deubiquitylating enzymes and drug discovery: emerging opportunities

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Keywords: GSK2643943A supplier, Deubiquitinase, inhibitors, activators


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