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5.31370

BMP-2 Signaling Enhancer, A01

Name: BMP-2 Signaling Enhancer, A01
Brand: MM

别名:

BMP-2 Signaling Enhancer, A01, (4-((4-Chloro-3-(trifluoromethyl)phenyl)sulfonyl)-1-piperazinyl)(4-(5-methyl-1H-pyrazol-1-yl)phenyl)methanone, Smurf1 Inhibitor, A01

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关于此项目

经验公式（希尔记法）:

C₂₂H₂₀ClF₃N₄O₃S

分子量:

512.93

MDL number:

MFCD00489974

UNSPSC Code:

12352200

NACRES:

NA.77

PubChem Substance ID:

2834965

Form:

powder

Assay:

≥97% (HPLC)

Solubility:

DMSO: 50 mg/mL

Color:

yellow

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属性

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

InChI

1S/C17H21N7O4/c25-24(26)14-3-1-13(2-4-14)18-15-19-16(22-5-9-27-10-6-22)21-17(20-15)23-7-11-28-12-8-23/h1-4H,5-12H2,(H,18,19,20,21)

InChI key

MSSXBKQZZINCRI-UHFFFAOYSA-N

说明

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).

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c