2080410-41-7
2080410-41-7 structure
- Name: GSK3494245
- Chemical Name: GSK3494245
- CAS Number: 2080410-41-7
- Molecular Formula: C21H23FN6O2
- Molecular Weight: 410.44
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Proteasome
- Create Date: 2022-03-23 15:02:03
- Modify Date: 2024-01-09 18:56:30
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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].
| Name | GSK3494245 |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| In Vitro | GSK3494245 shows EC50 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; EC50 > 50 μM)[1]. GSK3494245 (DDD01305143) shows pEC50s 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[2]. |
| 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)[1]. |
| References |
| Molecular Formula | C21H23FN6O2 |
|---|---|
| Molecular Weight | 410.44 |