GSK2556286

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].

Product Specifications

CAS Number

[1210456-20-4]

Product Name Alternative

GSK286

UNSPSC

12352005

Target

Bacterial

Type

Reference compound

Related Pathways

Anti-infection

Applications

COVID-19-immunoregulation

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gsk2556286.html

Purity

99.70

Solubility

DMSO : 3.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1C=C(CN2CCC(CC2)OC3=CC=CC(C)=C3C)NC(N1)=O

Molecular Formula

C18H23N3O3

Molecular Weight

329.39

References & Citations

[1]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.|[2]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.|[3]Vladimir Finger, et al., Pyrimidine derivatives with antitubercular activity, European Journal of Medicinal Chemistry, Volume 246, 2023, 114946, ISSN 0223-5234.