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.

ATX inhibitor 1 is a potent ATX inhibitor with IC50 values of 1.23 nM (FS-3) and 2.18 nM (bis-pNPP).

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

ATX-002 is a property-tunable lipid for RNA drug delivery.

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.

ATX-IN-1 (compound 35) is an ATX inhibitor with an IC50 of 0.7 nM, demonstrating anti-inflammatory properties. It effectively suppresses the TGF-β Smad pathway and reduces collagen deposition, alleviating fibrosis in a Bleomycin-induced mouse model. This compound also exhibits good oral bioavailability (F=69.5%) and microsomal stability.

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.

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].

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 21 is a potent inhibitor of ATX (IC50: 3490 nM).

ATX inhibitor 10 is a nitrogen-containing heterocyclic compound that is a potent inhibitor of ATX. Among other things, ATX plays a role in causing pathologies including fibrosis, neurodegeneration, arthritis, neuropathic pain, and cancer. ATX inhibitor 10 has shown research potential for ATX-related 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 12 is an orally active ATX inhibitor (IC50: 1.72 nM). In C57Bl 6J mice, oral administration of ATX inhibitor 12 at a dose of 60 mg kg was effective in inhibiting structural lung damage and reducing fibrotic lesions.

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

ATX inhibitor 20 is a potent inhibitor of ATX (IC50: 2.3 nM).

ATX inhibitor 14, an indole-based carbamate derivative, is a potent inhibitor (IC50: 0.41 nM) of self-adhesive proteins (ATX) and has shown potential for research in fibrosis-related diseases.

ATX inhibitor 19 is a potent inhibitor of ATX (IC50: 156 nM).

ATX inhibitor 16 is a potent ATX inhibitor (IC50: 0.0021 μM) that exhibits a significant anti-proliferative effect on breast cancer cells.

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.

ATX inhibitor 13 (compound 10c) is an orally active ATX inhibitor (IC50: 3.4 nM) that arrests the cell cycle of RAW264.7 cells in the G2 phase, inhibits cell proliferation and migration, induces apoptosis, and exhibits an inhibitory effect on tumour colony formation.

ATX inhibitor 17, a powerful ATX inhibitor, exhibits an IC50 value of 0.019 µM, demonstrating significant anti-proliferative effects in breast cancer cells.

ATX-II, an Na+ channel modulator toxin derived from the sea anemone (Anemonia sulcata), causes delayed inactivation of the Na+ channels and has been linked to pulmonary vein arrhythmogenesis and atrial fibrillation [1] [2]. It exhibits interaction with halothane, caffeine, and ryanodine.