NMS 873

Pricing Availability Delivery Time Qty
Cat.No. 6180 - NMS 873 | C27H28N4O3S2 | CAS No. 1418013-75-8
Description: Potent and selective p97 ATPase (VCP) allosteric inhibitor
Chemical Name: 3-[3-(Cyclopentylthio)-5-[[[2-methyl-4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]oxy]methyl]-4H-1,2,4-triazol-4-yl]pyridine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent p97 ATPase (VCP) allosteric inhibitor (IC50 = 30 nM). Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 μM). Activates the unfolded protein response (UPR) and modulates autophagosome maturation. Exhibits antiproliferative activity in cancer cells in vitro (IC50 values are 400 and 700 nM for HCT116 and HeLa cells respectively). Reduces p97-sensitization to trypsin digestion.

Technical Data

M. Wt 520.67
Formula C27H28N4O3S2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1418013-75-8
PubChem ID 71521142
InChI Key UJGTUKMAJVCBIS-UHFFFAOYSA-N
Smiles CC1=C(C2=CC=C(S(C)(=O)=O)C=C2)C=CC(OCC3=NN=C(N3C4=CN=CC=C4)SC5CCCC5)=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 52.07 100
ethanol 5.21 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 520.67. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.92 mL 9.6 mL 19.21 mL
5 mM 0.38 mL 1.92 mL 3.84 mL
10 mM 0.19 mL 0.96 mL 1.92 mL
50 mM 0.04 mL 0.19 mL 0.38 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 SDS / 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

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Magnaghi et al (2013) Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat.Chem.Biol. 9 548 PMID: 23892893

Anderson et al (2015) Targeting the AAA ATPase p97 as an approach to treat cancer through disruption of protein homeostasis. Cancer Cell 28 653 PMID: 26555175

Polucci et al (2013) Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J.Med.Chem. 56 437 PMID: 23245311


If you know of a relevant reference for NMS 873, please let us know.

View Related Products by Product Action

View all p97 ATPase Inhibitors

Keywords: NMS 873, supplier, NMS873, Potent, selective, valosine, containing, protein, VCP, p97, allosteric, inhibitors, inhibits, unfolded, protein, response, UPR, autophagosome, maturation, antiproliferative, anticancer, p97, ATPase, Tocris Bioscience

Citations for NMS 873

Citations are publications that use Tocris products.

Currently there are no citations for NMS 873. Do you know of a great paper that uses NMS 873 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Pathways for NMS 873

Protocols

TODO: Add Protocols