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GSK3186899

Catalog No. T15438 CAS 1972617-87-0

Synonyms: 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide, DDD-853651

GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.

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GSK3186899, CAS 1972617-87-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 297.00
5 mg	In stock	$ 647.00
10 mg	In stock	$ 987.00
25 mg	In stock	$ 1,470.00
50 mg	In stock	$ 1,990.00
100 mg	In stock	$ 2,680.00

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Purity: 98.35%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK3186899 is an inhibitor of Cdc2-related kinase 12 with an EC50 of 1.4 μM for L. donovani.
In vitro	GSK3186899 is active in cidal axenic amastigote assay with an EC50 value of 0.1 μM. GSK3186899 shows good selectivity against mammalian THP-1 host cells (EC50 value > 50 μM). GSK3186899 exhibits a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is more active using human peripheral blood mononuclear cells as the host cells[1].
In vivo	In the mouse model of infection, GSK3186899 (25 mg/kg; orally) reduces parasite levels by 99%. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). There are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested[1].

Synonyms	3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide, DDD-853651
Molecular Weight	491.53
Formula	C19H28F3N7O3S
CAS No.	1972617-87-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mg/mL (406.89 mM), Sonication is recommended.

References and Literature

1. Wyllie S, et al. Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis. Nature. 2018 Aug;560(7717):192-197.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Parasitic Compound Library

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Related compounds with same targets

Antimalarial agent 29 Retro-2 Antimalarial agent 13 Levamisole hydrochloride Sarolaner Antileishmanial agent-24 Sulfadiazine sodium Beta-mangostin

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GSK3186899 1972617-87-0 Microbiology/Virology Parasite GSK 3186899 DDD 853651 3,3,3-trifluoro-N-[4-[[3-[(2R)-2-methylmorpholin-4-yl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]cyclohexyl]propane-1-sulfonamide GSK-3186899 DDD-853651 DDD853651 inhibitor inhibit

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