Chemical Structure : GSK3186899
CAS No.: 1972617-87-0
Catalog No.: PC-35894Not For Human Use, Lab Use Only.
GSK3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).
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GSK3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).
GSK3186899 also shows activity against L. donovani axenic amastigotes with EC50 of 17 nM.
GSK3186899 demonstrates efficacy mouse model of visceral leishmaniasis.
M.Wt | 491.534 | |
Formula | C19H28F3N7O3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
1-Propanesulfonamide, 3,3,3-trifluoro-N-[trans-4-[[3-[(2S)-2-methyl-4-morpholinyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]- |
1. Wyllie S, et al. Nature. 2018 Aug;560(7717):192-197.
2. Thomas MG, et al. J Med Chem. 2018 Dec 20. doi: 10.1021/acs.jmedchem.8b01218.
3. WIPO patent WO/2016/116563 (2016).
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