GSK3186899 ( 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 )

Catalog No. M26705 CAS No. 1972617-87-0

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Product Name

GSK3186899
Note

Research use only, not for human use.
Brief Description

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

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
Pathway

Microbiology/Virology
Target

Parasite
Recptor

HIV-1
Research Area

——
Indication

——

CAS Number

1972617-87-0
Formula Weight

491.5
Molecular Formula

C19H28F3N7O3S
Purity

>98% (HPLC)
Solubility

——
SMILES

C[C@H]1CN(CCO1)c1n[nH]c2nc(N[C@H]3CC[C@@H](CC3)NS(=O)(=O)CCC(F)(F)F)ncc12
Chemical Name

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1.Van Duyne R, et al. Effect of mimetic CDK9 inhibitors on HIV-1-activated transcription. J Mol Biol. 2013 Feb 22;425(4):812-29.

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