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NMS-859, ATPase VCP/p97 Inhibitor

NMS-859, ATPase VCP/p97 Inhibitor

$139.00
A potent and specific small molecule covalent inhibitor of the ATPase VCP/p97.
Catalog No. Unit Price Qty
M60148-2s 2mg solid $139.00

Details

Product Information
Molecular Weight: 349.79
Formula: C15H12ClN3O3S
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: 2-chloro-N-(3-((1,1-dioxidobenzo[d]isothiazol-3-yl)amino)phenyl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

NMS-859 is a potent and specific small molecule covalent inhibitor of the ATPase VCP/p97 (IC50 ~0.37 µM), identified by high-throughput screening. It is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. NMS-859 was active in a cell proliferation assay, with IC50 values of 3.5 μM and 3.0 μM in HCT116 and HeLa cell lines, respectively. NMS-859 covalently modifies VCP on the active site Cys522 and blocks ATP binding. NMS-859 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-859 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: 349.79
Formula: C15H12ClN3O3S
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: 2-chloro-N-(3-((1,1-dioxidobenzo[d]isothiazol-3-yl)amino)phenyl)acetamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

NMS-859 is a potent and specific small molecule covalent inhibitor of the ATPase VCP/p97 (IC50 ~0.37 µM), identified by high-throughput screening. It is very selective (IC50 >10 μM) against all of the AAA ATPases, HSP90 or the 53 kinases tested. NMS-859 was active in a cell proliferation assay, with IC50 values of 3.5 μM and 3.0 μM in HCT116 and HeLa cell lines, respectively. NMS-859 covalently modifies VCP on the active site Cys522 and blocks ATP binding. NMS-859 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-859 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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