A01

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Cat.No. 5397 - A01 | C22H20ClF3N4O3S | CAS No. 1007647-73-5
Description: High affinity Smurf1 inhibitor; enhances BMP signaling
Chemical Name: [4-[[4-Chloro-3-(trifluoromethyl)phenyl]sulfonyl]-1-piperazinyl][4-(5-methyl-1H-pyrazol-1-yl)phenyl]methanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

High affinity Smurf1 E3 ubiquitin ligase inhibitor (Kd = 3.7 nM). Attenuates Smurf1-mediated Smad 1/5 degradation and enhances BMP signaling. Potentiates BMP-2-induced osteoblastic activity in C2C12 myoblasts and MC3T3-E1 osteoblast precursor cells.

Technical Data

M. Wt 512.93
Formula C22H20ClF3N4O3S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1007647-73-5
PubChem ID 17555704
InChI Key QFYLTUDRXBNZFQ-UHFFFAOYSA-N
Smiles ClC1=C(C(F)(F)F)C=C(S(N2CCN(C(C3=CC=C(N4C(C)=CC=N4)C=C3)=O)CC2)(=O)=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.29 100

Preparing Stock Solutions

The following data is based on the product molecular weight 512.93. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.95 mL 9.75 mL 19.5 mL
5 mM 0.39 mL 1.95 mL 3.9 mL
10 mM 0.19 mL 0.97 mL 1.95 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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References

References are publications that support the biological activity of the product.

Cao et al (2014) Selective small molecule compounds increase BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. Sci.Rep. 4 4965 PMID: 24828823


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Keywords: A01, A01 supplier, A01, bone, morphogenetic, proteins, high, affinity, smurf1, e3, ubiquitin, ligase, inhibitors, inhibits, smad, osteoblasts, BMP, and, Other, Activin, Receptors, Ubiquitin, E3, Ligases, 5397, Tocris Bioscience

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