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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Parasite-GSK3186899
GSK3186899

Chemical Structure : GSK3186899

CAS No.: 1972617-87-0

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

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 491.534
分子式 C19H28F3N7O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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]-

参考文献

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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