SK 216

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Cat.No. 6187 - SK 216 | C29H29NO6Na2 | CAS No. 654080-03-2
Description: Plasminogen activator inhibitor-1 (PAI-1) inhibitor
Chemical Name: 2-[5-[[6-[5-(1,1-Dimethylethyl)-2-benzoxazolyl]-2-naphthalenyl]oxy]pentyl]propanedioic acid disodium salt
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Plasminogen activator inhibitor-1 (PAI-1) inhibitor. Inhibits VEGF-induced migration and tube formation in HUVECs. Also attenuates TGF-β dependent epithelial-mesenchymal transition and fibroblast to myofibroblast differentiation in vitro. Reduces size and weight of subcutaneous tumors, and inhibits metastasis and angiogenesis in vivo. Reduces bleomycin-induced pulmonary fibrosis in vivo. Orally bioavailable.

Technical Data

M. Wt 533.52
Formula C29H29NO6Na2
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 654080-03-2
Smiles CC(C)(C)C1=CC=C(OC(C2=CC(C=CC(OCCCCCC(C(O[Na])=O)C(O[Na])=O)=C3)=C3C=C2)=N4)C4=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 2.67 5 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 533.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 37.49 mL 187.43 mL 374.87 mL
0.25 mM 7.5 mL 37.49 mL 74.97 mL
0.5 mM 3.75 mL 18.74 mL 37.49 mL
2.5 mM 0.75 mL 3.75 mL 7.5 mL

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References

References are publications that support the biological activity of the product.

Omori et al (2016) Inhibition of plasminogen activator inhibitor-1 attenuates transforming growth factor-β-dependent epithelial mesenchymal transition and differentiation of fibroblasts to myofibroblasts. PLoS One. 11 e0148969 PMID: 26859294

Takayama et al (2016) Inhibition of PAI-1 limits tumor angiogenesis regardless of angiogenic stimuli in malignant pleural mesothelioma. Cancer Res. 76 3285 PMID: 27197170

Masuda et al (2013) SK-216, an inhibitor of plasminogen activator inhibitor-1, limits tumor progression and angiogenesis. Mol.Cancer Ther. 12 2378 PMID: 23990114


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