VCP/p97 inhibitor,selective and allosteric
CAS：1418013-75-8
分子式：C27H28N4O3S2
分子量：520.67
纯度：98%
存储：Store at -20°C

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].

参考文献:
[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.