2080410-41-7
Chemical Structure
GSK3494245
Synonym(s): DDD01305143
- CAS No.: 2080410-41-7
- Formula:C21H23FN6O2
- Molecular Weight:410.44
IUPAC Name: N-(4-fluoro-3-(3-morpholinoimidazo[1,2-a]pyrimidin-7-yl)phenyl)pyrrolidine-1-carboxamide
InChIKey: SAJUCKZZYFFICP-UHFFFAOYSA-N
SMILES: O=C(N1CCCC1)NC2=CC=C(F)C(C3=NC4=NC=C(N5CCOCC5)N4C=C3)=C2
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[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GSK3494245 | 98.56% | 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. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
