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GSK3494245

CAT: 0804-HY-127102-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-127102-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1

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