A01; A01(SMURF1 inhibitor)

For research purposes only

Cat. No BA18112015

Availability In Stock

Description of biological activity

AO1 is an inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1) that is a major regulator of bone morphogenetic protein (BMP) signaling [1]. AO1 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-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smuf1)

IUPAC Name: 1-[4-chloro-3-(trifluoromethyl)benzenesulfonyl]-4-[4-(5-methyl-1H-pyrazol-1-yl)benzoyl]piperazine

Chemical Formula: C22H20ClF3N4O3S

SMILES:
Cc1ccnn1-c1ccc(cc1)C(=O)N1CCN(CC1)S(=O)(=O)c1ccc(Cl)c(c1)C(F)(F)F

CAS Number: 1007647-73-5

Molecular Weight: 512.930

Purity: >98%

Appearance: a beige powder

Solubility: DMSO

STORAGE AND HANDLING

Storage: Store at +20°C (Enamine), +4-8°C (Aldrich), +4°C (Axon MedChem).

Stability: Stable under normal condition.

Shipping Conditions: Shipped at room temperature.

USE PROTOCOL

Soluble in DMSO at 5mg/ml (Aldrich), 13 mg/ml (Axon MedChem). 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. DOI: 10.1007/s00018-012-1170-7.
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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