atx (autotaxin)

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

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

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

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

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.

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

Autotaxin-IN-7 (45) is a pyridine-2-carboxylic acid derivative exhibiting sub-nanomolar inhibition of ATX (IC50 = 0.086 nM) and features excellent cardiac safety (hERG > 30 μM) with minimal toxicity to fibroblasts. It inhibits the TGF-β/Smad signaling pathway, reducing α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) can be used in pulmonary fibrosis research.

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. It effectively inhibits cell migration and collagen gel contraction. Additionally, ATX inhibitor 26 demonstrates significant antifibrotic activity, reducing collagen deposition in a Bleomycin (BLM)-induced pulmonary fibrosis model.

ATX inhibitor 27 (Compound 31) is an ATX inhibitor. It demonstrates IC50 values of 13 nM against human autotaxin (hATX) and 23 nM against lysophosphatidylcholine (LPC). By inhibiting the ATX enzyme, ATX inhibitor 27 reduces LPA levels in the body. This compound is applicable in research related to ATX-LPA-associated conditions such as inflammation, neurodegenerative disorders, and cancer.

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.

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

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].

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.