NMS-873抑制剂、激动剂(CAS号1418013-75-8)NMS-873是VCP/p97变构抑制剂,IC50为20 nM。 NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with IC50 value of 20 nM (Wild Type, 1 mM ATP).
IC50 value: 20 nM (Wild Type VCP, 1 mM ATP)
Target: VCP/p97
in vitro: In standard assay conditions, NMS-873 had an IC50 of 30 nM, which was unchanged at saturating ATP concentration. NMS-862, which has micromolar biochemical potency, did not have measurable antiproliferative activity (IC50 >10 μM), whereas the nanomolar activity of NMS-873 translated into a submicromolar antiproliferative IC50 in HCT116 (0.4 μM) and HeLa (0.7 μM)
cells. We measured IC50 values in the range of 0.08 μM to 2 μM for NMS-873 in a panel of tumor cell lines that suggested potent but somehow selective inhibitor activity in different tumor cell lines [1].
in vivo: