1229652-21-4

1229652-21-4 structure

Name: HA 130
Chemical Name: [4-[[4-[(Z)-[3-[(4-fluorophenyl)methyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]methyl]phenyl]boronic acid
CAS Number: 1229652-21-4
Molecular Formula: C₂₄H₁₉BFNO₅S
Molecular Weight: 463.28600
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2017-12-19 04:49:40
Modify Date: 2024-01-03 18:39:49
HA130 is a selective ATX (autotaxin) inhibitor with IC50 of 28 nM. IC50 value: 28 nM [2]Target: ATXin vitro: HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation. [1]in vivo: HA130 instantaneously lowers plasma levels of LPA in mice after intravenous administration. HA130 is an inhibitor of the enzymatic activity of ATX, slows T cell migration across lymph node HEVs. HA130 decreased the "outside HEVs/inside HEVs" ratio by 3-4-fold, compared to vehicle-treated animals vehicle (p < 0.01 for both PLNs and MLNs). [1]

Name	[4-[[4-[(Z)-[3-[(4-fluorophenyl)methyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]methyl]phenyl]boronic acid
Synonyms	MPP dihydrochloride B-[3-[[4-[[3-[(4-Fluorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]methyl]phenyl]boronic Acid 3-[(4-{[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden]methyl}phenoxy)methyl]benzeneboronic acid HA 150 HA130

Description	HA130 is a selective ATX (autotaxin) inhibitor with IC50 of 28 nM. IC50 value: 28 nM [2]Target: ATXin vitro: HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation. [1]in vivo: HA130 instantaneously lowers plasma levels of LPA in mice after intravenous administration. HA130 is an inhibitor of the enzymatic activity of ATX, slows T cell migration across lymph node HEVs. HA130 decreased the "outside HEVs/inside HEVs" ratio by 3-4-fold, compared to vehicle-treated animals vehicle (p < 0.01 for both PLNs and MLNs). [1]
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Cancer
References	[1]. Zhang Y, et al. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-3924. [2]. Bai Z, et al. Constitutive lymphocyte transmigration across the basal lamina of high endothelial venules is regulated by theautotaxin/lysophosphatidic acid axis. J Immunol. 2013 Mar 1;190(5):2036-2048.

1229652-27-0

137660-67-4

~64%

1229652-21-4

Precursor 1
137660-67-4
DownStream 0