- BrP-LPA acts as both an Autotaxin inhibitor (94% inhibition at 10 μM) and pan LPA receptor antagonist (LPA1: 1.5 μM, LPA2: 1.4 μM, LPA3: 1.2 μM, LPA4: 0.27 μM).
BrP-LPA inhibits the invasiveness of NIH3T3 ras ATX cells by 40% and decreases chemotaxis by 23%. BrP-LPA reduces the size of breast (MDA-MB-231), colon (HCT-116), and melanoma (B16F10)
tumors in mouse models. It also attenuates collagen-induced arthritis. PPARγ is not activated by BrP-LPA.
- HA130 is a boronic acid-based inhibitor of the lysoPLD activity of Autotaxin (ATX). HA130 is a potent (IC50 = 28 nM) reversible inhibitor which interacts with the oxygen in active site residue T210.
HA130 is selective against ATX and does not show any activity against NPP1, alkaline phosphatase, and phosphodiesterase at concentrations up to 10 μM. In addition, proteosomal chymotryptic,
caspase, and typtic activities were not affected. It also showed minimal toxicity against A2058, HEK293T, and HepG2 cell lines (TD50 = 105, 83, & 2.056 μM, respectively).
Plasma ATX activity was inhibited and circulating LPA levels decreased when administered to mice.
- PF-8380 is a potent Autotaxin (ATX) inhibitor (IC50 2.8 nM/101 nM purified enzyme/whole blood). Excessive activity of ATX is associated with numerous inflammatory conditions, cancer, and other diseases.
- Lysophosphatidic acid (LPA) produced by ATX stimulates cell proliferation through G-protein coupled receptors (LPA1-4). PF-8380 is orally bioavailable and effectively inhibits ATX in vivo reducing
LPA levels in serum and at the site of inflammation in a rat arthritis model. Can delivered orally with Order# B-0706-EC: "Oral Formulation Vehicle".
- Thio-ccPA is a stabilized analogue of carbacyclic phosphatidic acid (ccPA). It inhibits the lysoPLD activity of Autotaxin (ATX) and acts as an LPA1/3 receptor antagonist.
Thio-ccPA decreases the viability of B16F10, A375, and MeWo melanoma cell lines. Addition of endogenous LPA did not reverse the effects of Thio-ccPA in B16F10 cells.
Thio-ccPA decreased the number of pulmonary and non-pulmonary metastases in a B16F10 metastatic melanoma mouse model.
S32826 [4-(Tetradecanoylamino)benzyl]phosphonic acid disodium salt]
- S32826 is a potent inhibitor of the enzyme Autotaxin with an IC50 in the nanomolar range. S32826 is suitable for in vitro studies using purified components or cultured cells.
Due to its short circulation half-life, S32826 is not recommended for use in animal models.
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