NMS-859
| CAS No. | 1449236-96-7 | Cat. No. | BCP19908 |
| Name | NMS-859 | ||
| Synonyms | NMS859;NMS 859; | ||
| Formula | C15H12ClN3O3S | M. Wt | 349.79 |
| Description | NMS-859 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. | ||
| Pathways | Cell Cycle/DNA Damage | ||
| Targets | p97 | ||
Structure
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