NMS-873 --- ATPase VCP/p97 Inhibitor


Catalog No. size PriceQuantity
M60165-2S 2mg solid $141
M60165-10S 10 mg solid $570

Description

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.

Product information

CAS Number: 1418013-75-8

Molecular Weight: 520.67

Formula: C27H28N4O3S2

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

Smiles: CC1=CC(=CC=C1C1C=CC(=CC=1)S(C)(=O)=O)OCC1=NN=C(SC2CCCC2)N1C1=CN=CC=C1

InChiKey: UJGTUKMAJVCBIS-UHFFFAOYSA-N

InChi: InChI=1S/C27H28N4O3S2/c1-19-16-22(11-14-25(19)20-9-12-24(13-10-20)36(2,32)33)34-18-26-29-30-27(35-23-7-3-4-8-23)31(26)21-6-5-15-28-17-21/h5-6,9-17,23H,3-4,7-8,18H2,1-2H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 10 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

NMS-873 was used at 2.5-10 µM final concentration in various in vitro assays.

References:

  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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