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, phosphodiesterase, at concentrations up to 10 microM. 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, & 2056 µM respectively). Plasma ATX activity was inhibited and circulating LPA levels decreased when administered to mice.

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References

1) H.M.H.G. Albers et al. “Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation” Proc. Natl. Acad. Sci. USA, 2010, 107, 7257-7262.2) H.M.H.G. Albers et al. “Discovery and Optimization of Boronic Acid Based Inhibitors of Autotaxin” J.Med. Chem., 2010, 53, 4958-4967.

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Categories	Biochemical Reagents
Filter	Autotaxin, Inhibitor
CAS Number	1229652-21-4
Molecular Formula	C24H19BFNO5S
Molecular Weight (g/mol)	463.29
Purity	>95%
Storage	-20 °C or below

Echelon常用产品报价单产品名货号公司分类商城分类美金价Echelon/Anti-Rat F1-ATP Synthase Alpha Subunit Rabbit Polyclonal Antibody/100 UL/Z-RATPAZ-RATPA功能性抗体400.00Echelon/Biotinylated Anti-PtdIns(3,4)P2 IgG/50 UG/Z-B034Z-B034其它重组蛋白586.00Echelon/Goat anti-human Autotaxin antibody/10 UG/Z-P400Z-P400抗人83.00Echelon/PI4-Kinase beta (PI4Kb), active/5 UG/P32-102GP32-102G激酶226.00Echelon/1-Methylhistamine dihydrochloride/25 MG/B-0032B-0032其他试剂154.00Echelon/Neutral Sphingomyelinase Assay Service/10 SAMPLES/T-1800T-1800脂类663.00Echelon/PI3-K Beta Inhibitor Screening Service/60 Samples/T-1300B-4T-1300B-4脂质代谢研究3407.00Echelon/Cardiolipin Beads/100 UL/P-BCLPP-BCLP微球123.00Echelon/PI3-K Alpha Inhibitor Screening Service/40 SAMPLE/T-1300A-3T-1300A-3多肽2966.00Echelon/5′ PtdIns(3,4,5)P3 Phosphatase Activity Fluorescence Polarization Assay/EA KIT/K-1400K-1400其它检测试剂盒557.00echelon-inc/Sphingosine 1-Phosphate ELISA Kit/1ea/K-1900-1eaK-1900-1eaInhibitors夹心法ELISA1214.00