BMP-2 Signaling Enhancer, A01-Calbiochem

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一般描述

A cell-permeable phenylsulfonyl-piperazinyl compound that enhances BMP-2 associated signaling by selectively inhibiting Smurf1-mediated Smad1/5 ubiquitination and thereby prolonging the half life of Smad1 and 5. Directly and specifically blocks WW domains mediated Smurf1-Smad1/5 complex formation (K_d= 3.664 nM), but has no effect on Smurf2-Smad2 and Smurf2-Smad3 interaction. Increases Smad1/5 levels in cells pre-transfected wild type Smurf1, but not the C699A mutant Smurf1 lacking ubiquitin ligase activity. Does not affect the mRNA levels of Smad1 and Smad5. Also, has no effect on the level of Smad2/3, Smad4, ING2 and RhoA. Shown to potentiate BMP-2 induced osteoblastic differentiation of C2C12 cells (~ 2 ?M in 48 h).
A cell-permeable phenylsulfonyl-piperazinyl compound that enhances BMP-2 associated signaling by selectively inhibiting Smurf1-mediated Smad1/5 ubiquitination and thereby prolonging the half life of Smad1 and 5. Directly and specifically blocks WW domains mediated Smurf1-Smad1/5 complex formation (K_d= 3.664 nM), but has no effect on Smurf2-Smad2 and Smurf2-Smad3 interaction. Increases Smad1/5 levels in cells pre-transfected wild type Smurf1, but not the C699A mutant Smurf1 lacking ubiquitin ligase activity. Does not affect the mRNA levels of Smad1 and Smad5. Also, has no effect on the level of Smad2/3, Smad4, ING2 and RhoA. Shown to potentiate BMP-2 induced osteoblastic differentiation of C2C12 cells (~ 2 ?M in 48 h).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
Smurf1

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Cao, Y., et al. 2014.Sci. Rep.4,4965.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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