Autotaxin Inhibitor

Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC₅₀ of 131 nM and a K_i of 15 nM.

PF-8380 is a potent autotaxin inhibitor with an IC₅₀ of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

HA130 is a selective autotaxin (ATX) inhibitor with an IC₅₀ of 28 nM.

ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC₉₀ of 100 nM for ATX activity in mouse plasma.

BI-2545, a chemical probe, is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC₅₀s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively.

ATX inhibitor 18 is a potent ATX inhibitor with an IC₅₀ value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis.

PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC₅₀ of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with an IC₅₀ of 2.4 nM, compound 33, sourced from patent WO2018212534A1.

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC₅₀ of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.

Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc.

S32826 disodium is a potent autotaxin inhibitor, with an IC₅₀ of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes.

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC₅₀ of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.

PAT-347 is an inhibitor of autotaxin (ATX, ENPP-2). PAT-347 binds only to the hydrophobic channel of ATX, without occupying its hydrophobic pocket and catalytic site. PAT-347 blocks the binding of lysophosphatidylcholine (LPC) to the catalytic site of ATX.

Autotaxin-IN-6 (compound 23) is a potent autotaxin (ATX) inhibitor with an IC₅₀ value of 30 nM. Autotaxin-IN-6 can reduce cell migration. Autotaxin-IN-6 can be used for researching anticancer.

ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC₅₀ of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research.

Autotaxin-IN-4 (compound 51), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat idiopathic pulmonary fibrosis.

Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC₅₀ of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis.

S32826 is a potent autotaxin inhibitor, with an IC₅₀ of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes.

EL244 is a dua Autotaxin (ATX) (IC₅₀ = 50 nM) inhibitor and PPARγ (IC₅₀ = 1.3 μM; K_d = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC₅₀ = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.

ATX inhibitor 20 (compound 24) is a potent ATX (autotaxin) inhibitor, with an IC₅₀ of 2.3 nM.