NMS 873New
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.
| 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 |
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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.
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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
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