≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
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 ( IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC 50 : purified 26S=13 µM; enriched THP-1 extracts IC 50 =40µM). GSK3494245 exhibits attractive biological and biosafety properties.
In Vitro
GSK3494245 shows EC 50 value of 5.7 μM in L. donovani intramacrophage assay, where the amastigotes are cultured in differentiated THP-1 cells. GSK3494245 demonstrates good selectivity over mammalian cell growth inhibition (THP-1 cells; EC 50 > 50 μM). GSK3494245 (DDD01305143) shows pEC 50 s of 6.5 and 5.8 against axenic amastigote and ld InMac, respectively. Ld InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigote. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK3494245 (25 mg/kg; orally twice a day for 10 consecutive days) elicits a >95% reduction of parasite load in Infected mice ( L. donovani , LV9) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
| Isomeric SMILES | C1CCN(C1)C(=O)NC2=CC(=C(C=C2)F)C3=NC4=NC=C(N4C=C3)N5CCOCC5 |
|---|---|
| PubChem CID | 126571915 |
| Molecular Weight | 410.44 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
Download SDS →Lot-specific quality data. Enter your lot number to retrieve the exact COA.
Look up COA →Full quality attributes and acceptance criteria for this grade.
View spec sheet →| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Solubility | DMSO : 100 mg/mL (243.64 mM; Need ultrasonic) |
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