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Locostatin

Catalog No. T8823 CAS 133812-16-5

Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.

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Locostatin, CAS 133812-16-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 59.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 172.00
100 mg	In stock	$ 249.00
200 mg	In stock	$ 373.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.84%

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Description	Locostatin is a potent and cell permeable inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
In vitro	Locostatin treatment resulted in the activation of the mitogen-activated protein kinase (MAPK) signal pathway (ERK phosphorylation), providing a powerful validation of our targeting protocol.?Further, RKIP inhibition by locostatin reduces ECM components.?Moreover, the inhibition of RKIP by locostatin impaired cell proliferation and migration in both leiomyoma and myometrial cells.?Finally, locostatin treatment reduced GSK3β expression.?Therefore, even if the activation of MAPK pathway should increase proliferation and migration, the destabilization of GSK3β leads to the reduction of proliferation and migration of myometrial and leiomyoma cells[1].
In vivo	Compared to the CCl4 group, HYP (208.56 ± 6.12) μg/g, percentage of total collagen at overall region (1.91 ± 0.13), MMP-13/TIMP-1 (0.19 ± 0.01), MPO (1.45 ± 0.04) U/g, TGF-β (2652 ± 91.20), PDGF-AA (3897 ± 290.69), and E-selectin (1569 ± 66.48) in the liver tissues were decreased significantly in the locostatin-treated group[2].
Animal Research	Carbon tetrachloride (CCl4) was used to induce liver fibrosis in mice, and locostatin was injected intraperitoneally. Liver fibrosis was assessed by Masson and Sirius red staining, hydroxyproline (HYP) assay, and collagen percentage area. Collagen I, collagen III, and α-SMA were detected by RT-PCR and western blot. The levels of MMP-13, MMP-2, TIMP-1, and TIMP-2 were estimated by ELISA. Liver inflammation was evaluated by HE staining and immunohistochemistry; liver myeloperoxidase (MPO), superoxide dismutase, and malondialdehyde were measured by ELISA; and cytokines were by Mouse Cytokine Array Q4000[2]

Molecular Weight	245.27
Formula	C14H15NO3
CAS No.	133812-16-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMF: 5 mg/ml

DMSO: 5 mg/ml

ethanol: 10 mg/ml

References and Literature

1. A M J , Stefania Greco A , B M S I A , et al. Locostatin, a disrupter of Raf kinase inhibitor protein, inhibits extracellular matrix production, proliferation, and migration in human uterine leiomyoma and myometrial cells[J]. Fertility and Sterility, 2016, 106( 6):1530-1538. 2. Junji, Yuzi, Qiu, et al. Locostatin Alleviates Liver Fibrosis Induced by Carbon Tetrachloride in Mice.[J]. Digestive diseases and sciences, 2019.

Citations

1. Ye J J, Wei S L, Wei Y Y, et al.RKIP suppresses the influenza A virus‑induced airway inflammatory response via the ERK/MAPK pathway.International Journal of Molecular Medicine.2023, 51(1): 1-14.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Anti-Ovarian Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Prostate Cancer Compound Library MAPK Inhibitor Library NO PAINS Compound Library HIF-1 Signaling Pathway Compound Library Anti-Obesity Compound Library Kinase Inhibitor Library

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Keywords

Locostatin 133812-16-5 MAPK Raf inhibitor inhibit

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