1210456-20-4
Chemical Structure
GSK2556286
Synonym(s): GSK286
- CAS No.: 1210456-20-4
- Formula:C18H23N3O3
- Molecular Weight:329.39
IUPAC Name: 6-((2,4-dimethoxybenzyl)amino)-4-((8'-methyl-1',5'-dioxo-1',5'-dihydro-2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridin]-6'-yl)amino)nicotinic acid hydrochloride
InChIKey: AZOFJHATIPDIER-UHFFFAOYSA-N
SMILES: O=C1C=C(CN2CCC(CC2)OC3=CC=CC(C)=C3C)NC(N1)=O
Biological Activity: GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes[1][2][3].
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GSK2556286 | 99.70% | GSK2556286 (GSK286) is an orally active and cholesterol-dependent Mycobacterium tuberculosis inhibitor. GSK2556286 inhibits Mycobacterium tuberculosis inside infected macrophages (IC50 = 0.07 μM in THP-1 cells), in the presence of cholesterol. GSK2556286 acts via Rv1625c, a membrane-bound adenylyl cyclase in Mycobacterium tuberculosis. GSK2556286 is an Rv1625 agonist leading to increased cAMP and reduced cholesterol metabolism. GSK2556286 can be studied in research for antitubercular purposes. | ||||||||||||||||||||
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- [1]. Brown KL, et al., 2023. Cyclic AMP-Mediated Inhibition of Cholesterol Catabolism in Mycobacterium tuberculosis by the Novel Drug Candidate GSK2556286. Antimicrob Agents Chemother 67:e01294-22.
- [2]. Nuermberger EL, et al. GSK2556286 Is a Novel Antitubercular Drug Candidate Effective In Vivo with the Potential To Shorten Tuberculosis Treatment. Antimicrob Agents Chemother. 2022 May 24:e0013222. [Content Brief]
- [3]. Vladimir Finger, et al., Pyrimidine derivatives with antitubercular activity, European Journal of Medicinal Chemistry, Volume 246, 2023, 114946, ISSN 0223-5234.
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