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GSK3186899

Chemical Structure : GSK3186899

CAS No.: 1972617-87-0

GSK3186899 (GSK-3186899, DDD853651, DDD-853651)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 491.534
Formula C19H28F3N7O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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]-

References

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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