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Smurf1 inhibitor A01

Chemical Structure : Smurf1 inhibitor A01

CAS No.: 1007647-73-5

Smurf1 inhibitor A01

Catalog No.: PC-21766Not For Human Use, Lab Use Only.

Smurf1 inhibitor A01 is a specific small molecule inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) with Kd of 3.66 nM for interrupting Smurf1-Smad1 interaction, impairs Smurf1-mediated Smad1/5 degradation and stabilizes Smad1/5 protein level.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Smurf1 inhibitor A01 is a specific small molecule inhibitor of ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) with Kd of 3.66 nM for interrupting Smurf1-Smad1 interaction, impairs Smurf1-mediated Smad1/5 degradation and stabilizes Smad1/5 protein level.
Smurf1 inhibitor A01 does not affect the protein level of Smad2/3, Smad4, ING2 and the small guanosine triphosphatase RhoA.
Smurf1 inhibitor A01 does not interrupt Smurf2-Smad2 or Smurf2-Smad3 interactions.
Smurf1 inhibitor A01 (2 uM) enhances BMP signaling responsiveness in C2C12 and mouse pre-osteoblasts MC3T3-E1 cells, induces gene expression of ALP, osteocalcin and type I collagen (α1).
Smurf1 inhibitor A01 (10 uM) potentiates BMP-2 induced osteoblastic activity in both C2C12 and MC3T3-E1 cells, potentiates BMP-2 induced ALP enrichment.

Physicochemical Properties

M.Wt 512.93
Formula C22H20ClF3N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(4-((4-chloro-3-(trifluoromethyl)phenyl)sulfonyl)piperazin-1-yl)(4-(5-methyl-1H-pyrazol-1-yl)phenyl)methanone

References

1. Yu Cao, et al. Sci Rep. 2014 May 14:4:4965.

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