Description
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.
Product information
CAS Number: 1449236-96-7
Molecular Weight: 349.79
Formula: C15H12ClN3O3S
Chemical Name: 2-chloro-N-(3-((1,1-dioxidobenzo[d]isothiazol-3-yl)amino)phenyl)acetamide
Smiles: O=C(CCl)NC1=CC(=CC=C1)NC1=NS(=O)(=O)C2=CC=CC=C21
InChiKey: JWMFLBAPPIWNGG-UHFFFAOYSA-N
InChi: InChI=1S/C15H12ClN3O3S/c16-9-14(20)17-10-4-3-5-11(8-10)18-15-12-6-1-2-7-13(12)23(21,22)19-15/h1-8H,9H2,(H,17,20)(H,18,19)
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 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-859 was used at 2.5-10 µM final concentration in various in vitro assays.
References:
- 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.
Documents
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.