HA130 free base · Synonyms: ATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid

A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity…

For research use only. Not for human or veterinary use.

Target Phosphodiesterase (PDE)

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

HA130 structure

CAS No.: 1229652-21-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 430.00	BP-02328-50mg	In stock	Get quote
100 mg	USD 650.00	BP-02328-100mg	In stock	Get quote
250 mg	USD 989.00	BP-02328-250mg	In stock	Get quote
500 mg	USD 1,698.00	BP-02328-500mg	In stock	Get quote
1 g	Inquire	BP-02328-1g	In stock	Inquire
2 g	Inquire	BP-02328-2g	In stock	Inquire

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Description

A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 µM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826

Biological activity

HA130 instantaneously lowers plasma levels of LPA in mice after intravenous administration.HA130 completely blocks the ability of ATX to promote TEM (transendothelial migration). HA130 at 0.3 μM completely ablates the activity of ATX on TK1 uropod formation.

Identifiers

SMILES: OB(O)C1=CC=CC(COC2=CC=C(\C=C3/SC(=O)N(CC4=CC=C(F)C=C4)C3=O)C=C2)=C1
InChIKey: VTNKMYWFWQTEHE-XKZIYDEJSA-N

Specifications

MW (average): 463.2860
Formula: C₂₄H₁₉BFNO₅S
CAS No.: 1229652-21-4
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

Documents

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.

Same target

Search Phosphodiesterase (PDE)

Same research area

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