GSK3494245

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].

Product Specifications

CAS Number

[2080410-41-7]

Product Name Alternative

DDD01305143

UNSPSC

12352005

Target

Parasite; Proteasome

Type

Reference compound

Related Pathways

Anti-infection; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/gsk3494245.html

Purity

98.66

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H23FN6O2

Molecular Weight

410.44

References & Citations

[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.