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USP7/USP47 inhibitor 

Cat. No. M28037
USP7/USP47 inhibitor  Structure
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Biological Activity

USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.

Chemical Information
Molecular Weight 484.4
Formula C18H11Cl2N3O3S3
CAS Number 1247825-37-1
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
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] Kailing Pan, et al. Front Cell Dev Biol. Role of Ubiquitin-Specific Peptidase 47 in Cancers and Other Diseases

[2] Olof Engström, et al. Bioorg Med Chem Lett. Discovery of USP7 small-molecule allosteric inhibitors

[3] Pablo Palazón-Riquelme, et al. EMBO Rep. USP7 and USP47 deubiquitinases regulate NLRP3 inflammasome activation

[4] Jinhua Piao, et al. J Biochem. Expression, purification and enzymatic characterization of a recombinant human ubiquitin-specific protease 47

[5] Joseph Weinstock, et al. ACS Med Chem Lett. Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47

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