GSK3494245

$510$4,200

Products Details

Product Description

– 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[1][2].

Web ID

– HY-127102

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– COVID-19-immunoregulation

Molecular Formula

– C21H23FN6O2

References

– [1]Wyllie S, et al. Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition. Proc Natl Acad Sci U S A. 2019;116(19):9318-9323. |[2]Thomas MG, et al. Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis. J Med Chem. 2019;62(3):1180-1202.

CAS Number

– 2080410-41-7

Molecular Weight

– 410.44

Compound Purity

– 98.66

SMILES

– O=C(N1CCCC1)NC2=CC=C(F)C(C3=NC4=NC=C(N5CCOCC5)N4C=C3)=C2

Clinical Information

– Phase 1

Research Area

– Infection

Solubility

– DMSO : 100 mg/mL (ultrasonic)

Target

– Parasite;Proteasome

Pathway

– Anti-infection;Metabolic Enzyme/Protease

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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