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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
HA130 (HA-130) is a novel, potent and selective inhibitor of autotaxin (ATX, IC50 = 28 nM) with anticancer activity. HA130 inhibits the enzymatic activity of ATX, and slows T cell migration across lymph node HEVs in vivo. Ex vivo, HA130 blunts the TEM-promoting activity of ATX, paralleling its in vivo effects. Autotaxin (ATX) is an ectoenzyme that catalyzes the conversion of lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), a bioactive lipid and a close relative of sphingosine 1-phosphate.
ln Vitro |
The capacity of ATX to stimulate TEM (transendothelial migration) is totally inhibited by HA130. At 0.3 μM, HA130 totally eliminated ATX's activity on TK1 tail-foot formation [1].
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ln Vivo |
HEV migration of T cells across lymph nodes is slowed by HA130. Comparing animals treated with HA130 to those not, the "external HEV/internal HEV" ratio is lowered by 3–4 times [1]. When HA130 is injected subcutaneously, draining lymph nodes (LN) experience a notable increase in lymphocytes within the endothelial cell (EC) and sub-EC layers of HEV [2].
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References |
[1]. Zhang Y, et al. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-3924.
[2]. Bai Z, et al. Constitutive lymphocyte transmigration across the basal lamina of high endothelial venules is regulated by theautotaxin/lysophosphatidic acid axis. J Immunol. 2013 Mar 1;190(5):2036-2048. |
Molecular Formula |
C24H19BFNO5S
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Molecular Weight |
463.2858
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CAS # |
1229652-21-4
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SMILES |
OB(C1=CC=CC(COC2=CC=C(/C=C(SC(N3CC4=CC=C(F)C=C4)=O)/C3=O)C=C2)=C1)O
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InChi Key |
VTNKMYWFWQTEHE-XKZIYDEJSA-N
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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-
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Chemical Name |
(Z)-(3-((4-((3-(4-fluorobenzyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)methyl)phenyl)boronic acid
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Synonyms |
HA-130; HA130; HA 130
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 39 mg/mL (~84.18 mM)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1585 mL | 10.7924 mL | 21.5848 mL | |
5 mM | 0.4317 mL | 2.1585 mL | 4.3170 mL | |
10 mM | 0.2158 mL | 1.0792 mL | 2.1585 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
HA130 impedes T cell entry into lymph nodes.J Immunol.2012 Oct 15;189(8):3914-24. |
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Binding of ATX to T cells.J Immunol.2012 Oct 15;189(8):3914-24. td> |
ATX induces motility of na.J Immunol.2012 Oct 15;189(8):3914-24. td> |