1210456-20-4
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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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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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Primidolol | Primidolol (UK-11443), derived from Parmotrema perlatum, possesses antibacterial and antioxidant activities. Primidolol is also an orally active α/β Adrenergic Receptor blocker with antihypertensive activity. Primidolol can be used in research related to infections and cardiovascular diseases. | |||||||||||||||||||||
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Ifoxetine hemisulfate | Ifoxetine (CGP 15210G) hemisulfate is an inhibitor of 5-HT reuptake. Ifoxetine hemisulfate specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine hemisulfate inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine hemisulfate has antidepressant properties. | |||||||||||||||||||||
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Ifoxetine | Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties. | |||||||||||||||||||||
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HL-3-47 | HL-3-47 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease. | |||||||||||||||||||||
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HA-CD44 interaction inhibitor 2 | 99.36% | HA-CD44 interaction inhibitor 2 is a CD44 inhibitor that can inhibit the interaction between Hyaluronic acid (HA) (HY-B0633A) and CD44. HA-CD44 interaction inhibitor 2 acts as an antiproliferative agent against CD44+ cancer cells. HA-CD44 interaction inhibitor 2 can disrupt the integrity of cancer spheres and reduce cancer cell viability in a dose-dependent manner. HA-CD44 interaction inhibitor 2 is applicable for tumor research. | ||||||||||||||||||||
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AChE/BuChE-IN-4 | 99.66% | AChE/BuChE-IN-4(compound 4a) is a multitarget-directed AChE/BuChE inhibitor againstAChEandBuChE, with the IC50 of 2.08 and 7.41 μM. | ||||||||||||||||||||
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SAR407899 hydrochloride | 99.14% | SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. | ||||||||||||||||||||
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SAR407899 | 99.67% | SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation. | ||||||||||||||||||||
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H1R ligand-1 | H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics. | |||||||||||||||||||||
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ASP-9521 | 98.0% | ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3. | ||||||||||||||||||||
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References
- [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.
