BMP-2 SIGNALING ENHANCER A01 (C005B-229406)

General description

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 µM 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 µM in 48 h).

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

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Smurf1

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 512.93. Empirical Formula: C₂₂H₂₀ClF₃N₄O₃S. Assay: ≥. 97% (HPLC). Quality Level: 100. form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 50 . mg/mL. storage temp.: 2-8°C. SMILES string: C1COCCN1C2: NC(: NC(: N2)NC3: CC: C(C: C3)[N+](: O)[O-])N4CCOCC4. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.