A reversible autotaxin inhibitor
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HA-130

Item No. 10498

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
B-[3-[[4-[[3-[(4-fluorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]methyl]phenyl]-boronic acid
CAS Number
1229652-21-4
Molecular Formula
C24H19BFNO5S
Formula Weight
463.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMSO: 5 mg/mLEthanol: 0.5 mg/mL
λmax
239, 348 nm
SMILES
FC1=CC=C(CN2C(/C(SC2=O)=C/C3=CC=C(OCC4=CC=CC(B(O)O)=C4)C=C3)=O)C=C1
InChi Code
InChI=1S/C24H19BFNO5S/c26-20-8-4-17(5-9-20)14-27-23(28)22(33-24(27)29)13-16-6-10-21(11-7-16)32-15-18-2-1-3-19(12-18)25(30)31/h1-13,30-31H,14-15H2/b22-13-
InChi Key
VTNKMYWFWQTEHE-XKZIYDEJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $142

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    25 mg

    $196

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    Product Description

    HA-130 is a reversible inhibitor of autotaxin, completely blocking the hydrolysis of the substrate bis-pNPP with an IC50 value of 28 nM.1 It does not affect the activity of any proteasomal protease or related enzymes. HA-130 rapidly decreases plasma lysophosphatidic acid levels in mice when given intravenously (1 nM/g).1 HA-130 has been used to investigate the role of autotaxin in cells and animals.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Albers, H.M.H.G., Dong, A., van Meeteren, L.A., et al. Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation. Proc. Natl. Acad. Sci. USA 107(16), 7257-7262 (2010).

    2. Lai, S.-L., Yao, W.-L., Tsao, K.-C., et al. Autotaxin/Lpar3 signaling regulates Kupffer’s vesicle formation and left-right asymmetry in zebrafish. Development 139(23), 4439-4448 (2012).

    3. Vázquez-Medina, J.P., Dodia, C., Weng, L., et al. The phospholipase A2 activity of peroxiredoxin 6 modulates NADPH oxidase 2 activation via lysophosphatidic acid receptor signaling in the pulmonary endothelium and alveolar macrophages. The FASEB Journal 30(8), 2885-2898 (2016).

    4. Zhang, Y., Chen, Y.-C.M., Krummel, M.F., et al. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J. Immunol. 189(8), 3914-3924 (2012).