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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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Purity & Documentation Purity: >98% (HPLC)

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); also shows activity against L. donovani axenic amastigotes with EC50 of 17 nM; 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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