A17; A17(SMURF1 inhibitor)

For research purposes only

Cat. No BA17112015

Availability In Stock

Description of biological activity

A17 is an inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1) that is a major regulator of bone morphogenetic protein (BMP) signaling [1]. A17 strongly inhibits Smad1/5 ubiquitination mediated by Smuf1, increases BMP signal responsiveness and enhances BMP-2 induced osteoblastic activity [2].

Therapeutic area

Bone disorders

Biological target category

E3 ubiquitin ligases

TECHNICAL INFORMATION

1-ethyl-6-fluoro-4-oxo-7-[4-(3-phenylpropanoyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylic acid inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

IUPAC Name: 1-ethyl-6-fluoro-4-oxo-7-[4-(3-phenylpropanoyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylic acid

Chemical Formula: C25H26FN3O4

SMILES: CCn1cc(C(=O)O)c(=O)c2c1cc(N1CCN(CC1)C(=O)CCc1ccccc1)c(c2)F

Molecular Weight: 451.500

Purity: >98%

Appearance: pale yellow powder

Solubility: DMSO

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light.

Stability: Stable under normal condition.

Shipping Conditions: Shipped at room temperature.

USE PROTOCOL

Soluble in DMSO. If precipitate is observed, vortex for 5 minutes.

REFERENCES

1. Cao, Y. et al. Smurf1 tale: function and regulation of an ubiquitin ligase in multiple cellular networks. Cell. Mol. Life Sci. 2013, 70, 2305.
2. Cao, Y. et al. Selective Small Molecule Compounds Increase BMP-2 Responsiveness by Inhibiting Smurf1-mediated Smad1/5 Degradation. Sci. Rep. 2014, 4, 4965. DOI: 10.1038/srep04965.

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