autotaxin (atx)

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM) that reduces CCl4-induced hepatic fibrosis and exhibits anti-hepatic fibrosis effects.

Autotaxin-IN-3 is an inhibitor of Autotaxin (IC50 = 2.4 nM) which is responsible for the increase in lysophosphatidic acid in ascites and plasma.

Ziritaxestat (GLPG1690), an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.

CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 0.014 μM.

ONO-8430506 is an orally available, potent autotaxin (ATX) ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.

BIO-32546 (S-isomer) is a highly potent regulator of autotaxin (ATX) with an IC50 value of 1 nM.

Z-HA155 (CS-963) selectively and potently inhibits autotaxin with an IC50 of 5.7 nM.

BI-2545 is an autotaxin (ATX) inhibitor that significantly reduces LPA. For human ATX and rat ATX, the IC50s values are 2.2 nM and 3.4 nM , respectively.

KR-40795 is an effective inhibitor of ATX (autotaxin) with an IC50 of 0.13 μM. This compound plays a crucial role in liver diseases.

ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. It exhibits excellent in vitro metabolic stability, with a half-life (t1 2) of over 170 minutes. In a bleomycin-induced pulmonary fibrosis mouse model, ATX inhibitor 25 (administered orally) shows antifibrotic effects.

HA 155 (Autotaxin Inhibitor IV) is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.

HA130 is a selective ATX (autotaxin) inhibitor.

PAT-347 is a potent inhibitor of Autotaxin (ATX), a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline.

ATX inhibitor 7 is an autotaxin inhibitor that demonstrates good oral exposure.

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. It effectively inhibits ATX activity in vivo, suppresses the expression of pro-fibrotic genes, and exhibits protective effects in Bleomycin-induced lung fibrosis in mice [1].

Cudetaxestat (BLD-0409) is a potent, orally active autotaxin inhibitor.

ATX inhibitor 9 is a thickened heteroaryl derivative compound and a potent inhibitor of ATX. Among them Autotaxin (ATX), also known as ENPP2, is a secreted enzyme highly expressed mainly in lung cancer cells, bronchial epithelial cells and alveolar macrophages.ATX inhibitor 9 has research potential for cancer or fibrous degenerative diseases.

ATX inhibitor 22 is a novel ATX (autotaxin) inhibitor with an IC50 of 218.9 μM, and it lacks inhibitory activity against LPAR1.

ATX inhibitor 8 is an inhibitor of the autocrine motor factor Autotaxin (ATX).

ATX inhibitor 11 is a potent inhibitor of ATX (autotaxin) (IC50: 2.7 nM). ATX inhibitor 11 alleviates the severity of fibrotic tissue and effectively reduces the deposition of α-SMA, a biomarker of fibrosis, in a mouse model of fibrosis. ATX inhibitor 11 can be used to study lung fibrosis.

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.

Autotaxin-IN-6 (compound 23) is a potent inhibitor of autotaxin (ATX), exhibiting an IC50 of 30 nM, and attenuates cell migration with potential applications in anticancer research [1].

MEY-003, an Autotaxin (ATX) inhibitor, exhibits EC50 values of 460 nM for hATX-β and 1.09 μM for hATX-ɣ (analysis with LPC18:1), demonstrating its potency against these isoforms. It acts non-competitively with a K i of 432 nM, making it suitable for research into diseases where ATX is implicated [1].

Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) serves as a moderately effective autotaxin (ATX) inhibitor, exhibiting an IC50 value of 620 nM. This compound finds utility in melanoma research[1].