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Proteins and Peptides

HA130 (Autotaxin Inhibitor)

Product Sizes
5 mg
£168.00
ECH-B-0701-5MG
10 mg
£250.00
ECH-B-0701-10MG
About this Product
SKU:
ECH-B-0701
Extra Details:
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 uM respectively). Plasma ATX activity was inhibited and circulating LPA levels decreased when administered to mice. \n \n \n \nStorage \n-20°C \nReferences \n1) 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. \n2) H.M.H.G. Albers et al. "Discovery and Optimization of Boronic Acid Based Inhibitors of Autotaxin" J.Med. Chem., 2010, 53, 4958-4967. \n \n \n \nDocuments \nTechnical Data Sheet, Echelon
Shipping Conditions:
Ambient
Storage Conditions:
Please refer to datasheet
Supplier:
Echelon Biosciences
Type:
Proteins, Peptides, Small Molecules & Other Biomolecules: Inhibitors