atx (autotaxin)

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

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.

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.

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

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

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

HA130 is a selective ATX (autotaxin) inhibitor.

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

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.

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].

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

CBT-295, an orally active autotaxin (ATX) inhibitor, effectively decreases inflammatory cytokines including TGF-β, TNF-α, and IL-6, along with the bile duct proliferation marker CK-19, and ameliorates liver fibrosis. The compound's ability to reverse liver fibrosis contributes to lowered ammonia levels in the blood and brain, which in turn reduces ammonia-induced neuroinflammation. CBT-295 shows potential for the study of liver cirrhosis and related encephalopathy.

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.

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.

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

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.

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

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].

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

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].

MHC02181 is a powerful Autotaxin (ATX) inhibitor, exhibiting an IC50 of 9.41 μM [1].

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.

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.

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].