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Drug intelligence / Profile preview
HA130
- Development stage
- Unknown
- Modality
- Small Molecules
- Administration
- Intravenous, Oral, Subcutaneous
01
Overview
HA130 is a potent, selective, and reversible boronic acid-based inhibitor of autotaxin (ATX, also known as ectonucleotide pyrophosphatase/phosphodiesterase family member 2 or ENPP2) with an IC50 of approximately 28 nM. It targets the active site Thr210 of ATX via its boronic acid moiety, blocking its lysophospholipase D (lysoPLD) activity and thereby preventing the conversion of lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA). HA130 is widely used as a research tool to study the LPC-ATX-LPA signaling axis, which is implicated in inflammation, fibrosis, cancer cell migration, and immune cell homing.
- Other names
- Autotaxin Inhibitor IIB-[3-[[4-[[3-[(4-fluorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]methyl]phenyl]-boronic acidCAS 1229652-21-4CAS1229652-21-4CAS-1229652-21-4
02
Targets
ENPP2 (Ectonucleotide pyrophosphatase/phosphodiesterase family member 2)
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