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NMS-873, ATPase VCP/p97 Inhibitor

NMS-873, ATPase VCP/p97 Inhibitor

$139.00
A potent and specific small molecule allosteric inhibitor of the ATPase VCP/p97.
Catalog No. Unit Price Qty
M60165-2s 2mg solid $139.00

Details

Product Information
Molecular Weight: 520.67
Formula: C27H28N4O3S2
Purity: ≥98%
CAS#: 1418013-75-8
Solubility: DMSO up to 100 mM
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
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

NMS-873 is a potent and specific small molecule allosteric inhibitor of the ATPase VCP/p97 (IC50 ~0.03 µM), identified by a high-throughput screening. It is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. Using photo-affinity labeling, structural analysis and mutagenesis, the binding site of NMS-873 was found to be a region spanning the D1 and D2 domains of adjacent protomers encompassing elements important for nucleotide-state sensing and ATP hydrolysis. NMS-873 activated the unfolded protein response, interfered with autophagy, and induced cancer cell death. NMS-873 provided critical validation of VCP as a cancer target, and it raises the possibility that targeting VCP might prevent proteasome inhibitor–resistant tumors from escaping through the aggresome-autophagy pathways and cause them to collapse under the high load of unfolded proteins. 

 

How to Use:

  • In vitro:  NMS-873 was used at 2.5-10 µM final concentration in various in vitro assays. 
  • In vivo: n/a

 

Reference:

  1. 1. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. (2013) Nat Chem Biol. 9(9):548-56
 

 

Products are for research use only. Not for human use.

 

Description

Details

Product Information
Molecular Weight: 520.67
Formula: C27H28N4O3S2
Purity: ≥98%
CAS#: 1418013-75-8
Solubility: DMSO up to 100 mM
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
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

NMS-873 is a potent and specific small molecule allosteric inhibitor of the ATPase VCP/p97 (IC50 ~0.03 µM), identified by a high-throughput screening. It is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. Using photo-affinity labeling, structural analysis and mutagenesis, the binding site of NMS-873 was found to be a region spanning the D1 and D2 domains of adjacent protomers encompassing elements important for nucleotide-state sensing and ATP hydrolysis. NMS-873 activated the unfolded protein response, interfered with autophagy, and induced cancer cell death. NMS-873 provided critical validation of VCP as a cancer target, and it raises the possibility that targeting VCP might prevent proteasome inhibitor–resistant tumors from escaping through the aggresome-autophagy pathways and cause them to collapse under the high load of unfolded proteins. 

 

How to Use:

  • In vitro:  NMS-873 was used at 2.5-10 µM final concentration in various in vitro assays. 
  • In vivo: n/a

 

Reference:

  1. 1. Magnaghi P, et al. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. (2013) Nat Chem Biol. 9(9):548-56
 

 

Products are for research use only. Not for human use.

 

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