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GSK3494245

Cat. No. M29173

All AbMole products are for research use only, cannot be used for human consumption.

GSK3494245 Structure
Synonym:

DDD01305143​

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Quality Control & Documentation
Biological Activity

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.

Chemical Information
Molecular Weight 410.44
Formula C21H23FN6O2
CAS Number 2080410-41-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Mohd Imran, et al. Expert Opin Ther Pat. Small molecules as kinetoplastid specific proteasome inhibitors for leishmaniasis: a patent review from 1998 to 2021

[2] Michael Thomas, et al. J Med Chem. Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis

[3] Susan Wyllie, et al. Proc Natl Acad Sci U S A. Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

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Keywords: GSK3494245, DDD01305143​ supplier, Parasite, inhibitors, activators

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