Home / Pharmacology / Enzymes / Ligases / Ubiquitin E3 Ligases / Ubiquitin E3 Ligase Inhibitors / A01

A01

Cat. No. 5397 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for A01

A01 is a 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 for A01

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A01

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

Preparing Stock Solutions for A01

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

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References for A01

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

If you know of a relevant reference for A01, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Ubiquitin E3 Ligase Inhibitors

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

Citations for A01

Citations are publications that use Tocris products.

Currently there are no citations for A01. Do you know of a great paper that uses A01 from Tocris? Please let us know.

Reviews for A01

There are currently no reviews for this product. Be the first to review A01 and earn rewards!

Have you used A01?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Programmed Cell Death Poster

Programmed Cell Death Poster

There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.

Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia