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NIH-12848

Names

[ CAS No. ]:
959551-10-1

[ Name ]:
NIH-12848

[Synonym ]:
N-(thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine

Biological Activity

[Description]:

NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC50 of 1 μM.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Cardiovascular Disease

[Target]

IC50: 1 μM (PI5P4Kγ)[1]


[In Vitro]

NIH-12848 inhibits PI5P4Kγ with an IC50 of approximately 1 μM but does not inhibit the α and β PI5P4K isoforms at concentrations up to 100 μM. NIH-12848 inhibits the translocation of Na+/ K+-ATPase to the plasma membrane that occurs when mpkCCD cells grow to confluence and also prevents reversibly their forming of ‘domes’ on the culture dish. Both these NIH-12848-induced effects are mimicked by specific RNAi knockdown of PI5P4Kγ, but not that of PI5P4Ks α or β. NIH-12848 could be a potentially powerful tool for exploring the cell physiology of PI5P4Ks[1].

[References]

[1]. Clarke JH, et al. The function of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) explored using a specific inhibitor that targets the PI5P-binding site. Biochem J. 2015 Mar 1;466(2):359-67.


[Related Small Molecules]

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline

Chemical & Physical Properties

[ Molecular Formula ]:
C20H14F3N3S

[ Molecular Weight ]:
385.412

[ Appearance of Characters ]:
white solid

[ Storage condition ]:
-20℃


Related Compounds