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Submit ReviewHA 130
Description: Potent and selective autotaxin inhibitor
Chemical Name: B-[3-[[4-[[3-[(4-Fluorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]methyl]phenyl]-boronic acid
Purity: ≥98% (HPLC)
Biological Activity for HA 130
HA 130 is a potent and selective autotaxin inhibitor (IC50 = 28 nM). Binds and inhibits autotaxin reversibly. Displays no activity against the proteasome, recombinant NPP1 or alkaline phosphatase. Inhibits ATX-mediated cell migration in an A2058 melanoma cell assay.
Compound Libraries for HA 130
HA 130 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for HA 130
| M. Wt | 463.29 |
| Formula | C24H19BFNO5S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1229652-21-4 |
| PubChem ID | 46911532 |
| InChI Key | VTNKMYWFWQTEHE-XKZIYDEJSA-N |
| Smiles | FC1=CC=C(CN3C(/C(SC3=O)=C/C2=CC=C(OCC4=CC(B(O)O)=CC=C4)C=C2)=O)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for HA 130
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.33 | 100 |
Preparing Stock Solutions for HA 130
The following data is based on the product molecular weight 463.29. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.16 mL | 10.79 mL | 21.58 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.32 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets for HA 130
References for HA 130
References are publications that support the biological activity of the product.
Albers et al (2010) Discovery and optimization of boronic acid based inhibitors of autotaxin. J.Med.Chem. 53 4958 PMID: 20536182
Albers et al (2010) Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation. Proc.Natl.Acad.Sci.USA 107 7257 PMID: 20360563
If you know of a relevant reference for HA 130, please let us know.
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Keywords: HA 130, HA 130 supplier, HA130, autotaxin, inhibitors, reversible, reversibly, inhibits, selective, atx, npp2, lysophospholipases, d, lysopld, Autotaxin, 4196, Tocris Bioscience
2 Citations for HA 130
Citations are publications that use Tocris products. Selected citations for HA 130 include:
Sandeep et al (2012) Exocrine pancreatic carcinogenesis and autotaxin expression. PLoS One 7 e43209 PMID: 22952646
Wheeler et al (2015) The Autotaxin-Lysophosphatidic Acid Axis Modulates Histone Acetylation and Gene Expression during Oligodendrocyte Differentiation. J Neurosci 35 11399 PMID: 26269646
Do you know of a great paper that uses HA 130 from Tocris? Please let us know.
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