autotaxin

Autotaxin-IN-3 是 Autotaxin 的抑制剂(IC50 = 2.4 nM)，Autotaxin 负责增加腹水和血浆中的溶血磷脂酸。

HA 155 (Autotaxin Inhibitor IV) 是一种基于硼酸的化合物，通过选择性结合其催化苏氨酸来抑制 ATX，IC50 为 5.7 nM。

ATX inhibitor 5 是一种有效且具有口服活性的 autotaxin (ATX) 抑制剂（IC50 ： 15.3 nM），可降低 CCl4 诱导的肝纤维化水平，具有抗肝纤维化作用，。

Ziritaxestat (GLPG1690) 是一种创新的 autotaxin (ATX)抑制剂，其 IC50=131 nM，Ki=15 nM。

Cudetaxestat (BLD-0409) 是口服具有活力的autotaxin 的有效抑制剂。

HA130 是选择性 autotaxin 抑制剂，IC50=28 nM。

CRT0273750 是一种 ATX 抑制剂的先导化合物，可调节血浆中 LPA 水平，用于 ATX LPA 依赖性癌症模型。

Z-HA155 (CS-963) 是一种高效的 ATX 选择性抑制剂，其 IC50=5.7 nM。

PF8380 是有效的autotaxin 抑制剂，在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。

ONO-8430506 是一种可口服的、具有有效性的 autotaxin (ATX) ENPP2 抑制剂（ IC90 ：100 nM），能够抑制小鼠血浆中 ATX 活性。

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

Autotaxin-IN-6 (compound 23)，一种ATX (自分泌运动分子)抑制剂，具有30 nM的IC50值，能够减少细胞迁移，适用于抗癌研究。

Autotaxin modulator 1 is a new modulator of Autotaxin.

Autotaxin-IN-5 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK PD relationship and it is used in treatment of osteoarthritis pain[1].

ATX inhibitor 22 是 ATX (autotaxin) 的新型抑制剂 (IC50: 218.9 μM)，对 LPAR1 缺乏抑制活性。

PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma.

Sphingomyelins are complex membrane lipids composed of phosphorylcholine, sphingosine, and an acylated group, such as a fatty acid. Lysosphingomyelin is a naturally-occurring lipid which is produced by the removal of the acylated group of sphingomyelin by a deacylase. Lysosphingomyelin may, in turn, serve as a substrate for autotaxin, which removes choline to produce sphingosine-1-phosphate. The receptors and signaling pathways that are activated by lyso-sphingosine are diverse and vary between cell types. Lysosphingomyelin occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases, including dermatitis and Niemann-Pick disease.

MEY-003是针对Autotaxin(ATX)的抑制剂，具有对hATX-β和hATX-ɣ的EC50值分别为460 nM和1.09 μM（LPC18:1分析条件下）。作为一种非竞争性抑制剂，其Ki值为432 nM。该化合物主要应用于ATX相关疾病的研究领域。

autotaxin inhibitor

PAT-505 是一种可口服且具有选择性和高效性的自体表皮生长因子抑制剂（在 Hep3B 细胞中的 IC50 为 2 nM，在人体血液中的 IC50 为 9.7 nM，在小鼠血浆中的 IC50 为 62 nM）。

BIO-32546 (S-isomer) 是一种高效的 autotaxin (ATX) 的调节剂，IC50 值为 1 nM。

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 是 ATX (autotaxin) 的有效抑制剂 (IC50: 2.7 nM)。ATX inhibitor 11 能够缓解小鼠纤维化模型中纤维化组织的严重程度，有效减少纤维化生物标志物 α-SMA 的沉积。ATX inhibitor 11 能够用于研究肺纤维化。

PAT-078 is an inhibitor of type II autotaxin.

ATX inhibitor 7 is a autotaxin inhibitor and shows 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. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1].

ATX inhibitor 8 是自分泌运动因子 Autotaxin (ATX) 抑制剂。

PF-8380 hydrochloride 是一种有效的autotaxin 抑制剂，体外酶实验和人类全血细胞实验中，IC50分别为 2.8 nM 和 101 nM。

PAT-494 is an inhibitor of type II Autotaxin.

MHC02181, 作为一种高效Autotaxin(ATX)抑制剂，其半抑制浓度IC50达到9.41 μM。

S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes.

BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.

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.

ATX inhibitor 9 是增稠的杂芳基衍生物化合物，也是 ATX 的有效抑制剂。其中 Autotaxin (ATX)，也称为 ENPP2，是一种主要在肺癌细胞、支气管上皮细胞和肺泡巨噬细胞中高度表达的分泌酶。ATX inhibitor 9 对癌症或纤维退行性疾病具有研究潜力。

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.

MHC00188 是变构抑制剂，针对自分泌运动因子 (ATX)，具有IC50值为2.53 μM。

Cyclic Phosphatidic Acids (cPAs) are naturally occurring lysophosphatidic acid (LPA) analogs, characterized by a 5-membered ring formed between the sn-2 hydroxy group and the sn-3 phosphate. Carba-derivatives of cPA (ccPA) modify the sn-2 (2-ccPA) or sn-3 (3-ccPA) linkage, hindering the conversion of cPA into LPA. Oleoyl 3-Carbacyclic Phosphatidic Acid (3-ccPA 18:1) incorporates the 18:1 fatty acid oleate at the sn-1 position on the glycerol backbone, acting as a cyclic LPA analog. This compound, at a concentration of 25 μM, blocks MM1 cells' transcellular migration through mesothelial cell monolayers induced by fetal bovine serum (by 90.1%) or LPA (by 99.9%), without impeding cell proliferation. Additionally, 3-ccPA 18:1, in the 0.1-1.0 μM range, notably suppresses autotaxin, which plays a vital role in various cancer cell behaviors including survival, growth, migration, invasion, and metastasis.

Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) 作为一种autotaxin (ATX) 抑制剂，具有中等效力，IC50值为620 nM。该化合物适用于黑色素瘤的研究。