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NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM. NMS-873 has antiproliferative effect on a panel of tumor cell lines with IC50 values in the range of 0.08 μM to 2 μM. For HCT116 and HeLa cells, the IC50 values are 0.4 μM and 0.7 μM, respectively. NMS-873 reduces VCP sensitivity to trypsin digestion, preventing degradation of the linker-D2 domain.
Nature. 2017 Dec 6.
Alcohol-abuse drug disulfiram targets cancer via p97 segregase adaptor NPL4
NMS-873 purchased from AbMole
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Source | Nature (2017). Figure 6. NMS873 (Abmole Bioscience) |
| Method | Western blot | |
| Cell Lines | NIH3T3 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 3 h | |
| Results | In contrast to treatment with NMS873, CuET had no effect on p97 ATPase activity |
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Source | Nature (2017). Figure 4. NMS873 (Abmole Bioscience) |
| Method | Western blot | |
| Cell Lines | NIH3T3 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 3 h | |
| Results | We confirmed UPR in cells treated with CuET or NMS873 by detecting increased markers of UPR induction, including the spliced form of XBP1s, ATF4 and phosphorylated (p-) eIF2α33 |
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Source | Nature (2017). Figure 2. NMS873 (Abmole Bioscience) |
| Method | colony-formation assay | |
| Cell Lines | U2OS cell | |
| Concentrations | 10 μM | |
| Incubation Time | 16 h | |
| Results | Furthermore, consistent with cleavage of the 120-kDa species of the endoplasmic reticulum-tethered transcription factor NRF1 into an active 110-kDa form being a p97-dependent process30, appearance of the cleaved NRF1 form was inhibited by both CuET and NMS873 |
| Molecular Weight | 520.67 |
| Formula | C27H28N4O3S2 |
| CAS Number | 1418013-75-8 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related p97 Products |
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| CB-5339
CB-5339 is a potent p97 inhibitor with an IC50 <30 nM (WO2015109285A1, compound FF07). |
| CB-5083
CB-5083 is a first-in-class, potent and selective, orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM. |
| DBeQ
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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