Name: NMS-873
Price: 276.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    NMS-873 is a selective inhibitor of VCP with IC50 value of 30nM [1].
    NMS-873 is the most potent and specific VCP inhibitor. It shows similar potency against both wild-type VCP and VCPC522T without affecting the oligomeric state of VCP. NMS-873 is selective against all of the AAA ATPases, HSP90 or some other kinases. The inhibition effect of NMS-873 is potent and somehow selective in a panel of tumor cell lines when its concentration ranges from 0.08μM to 2μM. NMS-873 suppresses cell proliferation in HCT-116 cell line through inducing accumulation of poly-Ub proteins and stabilization of cyclin E and Mcl-1 dose-dependently. Additionally, NMS-873 causes distribution of HCT116 cells, leading a dose and time-dependent increase in the G2 population and in the sub-G1 fraction. Further, NMS-873 shows cell killing activity in hematological tumors as well as a wide variety of solid tumors with IC50 range between 0.08μM and 2μM [1].
    
    [1] Magnaghi P, D'Alessio R, Valsasina B, Avanzi N, Rizzi S, Asa D, Gasparri F, Cozzi L, Cucchi U, Orrenius C, Polucci P, Ballinari D, Perrera C, Leone A, Cervi G, Casale E, Xiao Y, Wong C, Anderson DJ, Galvani A, Donati D, O'Brien T, Jackson PK, Isacchi A. Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat Chem Biol. 2013 Sep;9(9):548-56. doi: 10.1038/nchembio.1313. Epub 2013 Jul 28.
- Properties
  - Alternative Name
    
    3-[3-cyclopentylsulfanyl-5-[[3-methyl-4-(4-methylsulfonylphenyl)phenoxy]methyl]-1,2,4-triazol-4-yl]pyridine
    
    CAS Number
    
    1418013-75-8
    
    Molecular Formula
    
    C27H28N4O3S2
    
    Molecular Weight
    
    520.67
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥17.1 mg/mL in DMSO; ≥2.54 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Rycenga HB, Wolfe KB, et al. "Uncoupling of p97 ATPase activity has a dominant negative effect on protein extraction." Sci Rep. 2019 Jul 17;9(1):10329. PMID:31316150
    2. McLelland GL, Goiran T, et al. "Mfn2 ubiquitination by PINK1/parkin gates the p97-dependent release of ER from mitochondria to drive mitophagy." Elife. 2018 Apr 20;7. pii: e32866. PMID:29676259
    3. Yeo SK, French R, et al. "Opposing roles of Nfkb2 gene products p100 and p52 in the regulation of breast cancer stem cells." Breast Cancer Res Treat. 2017 Apr;162(3):465-477. PMID:28190248
    4. Fullbright G, Rycenga HB, et al. "p97 Promotes a Conserved Mechanism of Helicase Unloading during DNA Cross-Link Repair." Mol Cell Biol. 2016 Nov 14;36(23):2983-2994. PMID:27644328

NMS-873

NMS-873

Background

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