HA155

Names

[ Name ]:
HA155

[Synonym ]:
Boronic acid,B-[4-[[4-[(Z)-[3-[(4-fluorophenyl)Methyl]-2,4-dioxo-5-thiazolidinylidene]Methyl]phenoxy]Methyl]phenyl]-

Biological Activity

[Description]:

HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM[1][2][3].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Inflammation/Immunology

[Target]

IC50: 5.7 nM (ATX)[1]

[In Vitro]

HA-155 inhibits ATX by binding to the ATX active site[1]. HA155 completely attenuates the thrombin-mediated increase in platelet-derived LPA in a dose-dependent manner[3].

[References]

[1]. Albers HM, et al. Chemical Evolution of Autotaxin Inhibitors. Chem Rev. 2012 May 9;112(5):2593-603.

[2]. Albers HM, et al. Structure-based design of novel boronic acid-based inhibitors of autotaxin. J Med Chem. 2011 Jul 14;54(13):4619-26.

[3]. Fulkerson Z, et al. Binding of autotaxin to integrins localizes lysophosphatidic acid production to platelets and mammalian cells. J Biol Chem. 2011 Oct 7;286(40):34654-63.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₁₉BFNO₅S

[ Molecular Weight ]:
463.28600

[ Exact Mass ]:
463.10600

[ PSA ]:
112.37000

[ LogP ]:
3.25890

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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