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Formula | C27H28N4O3S2 |
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Molecular Weight | 520.67 | CAS No. | 1418013-75-8 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (192.06 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM). | ||
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In vitro | NMS-873 reduces p97 sensitivity to trypsin digestion, preventing degradation of the linker-D2 domain. NMS-873, as a p97 inhibitor, produces antiproliferative activity in a variety of hematological and solid tumor lines. The mechanism study indicates that NMS-873 activates the unfolded protein response, interfers with autophagy and thus induces cancer cell death. [1] | ||
Features | The most potent and specific p97 inhibitor described to date. |
Kinase Assay: |
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Cell Assay: |
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, , Toxicol Appl Pharmacol, 2016, 305:267-73.
Replication fork uncoupling causes nascent strand degradation and fork reversal [ Nat Struct Mol Biol, 2023, 30(1):115-124] | PubMed: 36593312 |
Replication fork uncoupling causes nascent strand degradation and fork reversal [ Nat Struct Mol Biol, 2023, 30(1):115-124] | PubMed: 36593312 |
K6-linked ubiquitylation marks formaldehyde-induced RNA-protein crosslinks for resolution [ Mol Cell, 2023, 10.1016/j.molcel.2023.10.011] | PubMed: 37951215 |
Actionable cancer vulnerability due to translational arrest, p53 aggregation and ribosome biogenesis stress evoked by the disulfiram metabolite CuET [ Cell Death Differ, 2023, 10.1038/s41418-023-01167-4] | PubMed: 37142656 |
Senescent cells form nuclear foci that contain the 26S proteasome [ Cell Rep, 2023, 42(8):112880] | PubMed: 37541257 |
Proteomics Profiling Reveals the Molecular Signatures and Potential Therapeutic Targets of Human Nasopharyngeal Carcinoma [ Mol Cell Proteomics, 2023, 22(6):100567] | PubMed: 37172717 |
Elucidating cellular interactome of chikungunya virus identifies host dependency factors [ Virol Sin, 2023, 38(4):497-507] | PubMed: 37182691 |
p97/VCP drives turnover of SUMOylated centromeric CCAN proteins and CENP-A [ Molecular Biology of the Cell, 2023, 34(5)] | PubMed: None |
Regulation of membrane fluidity by RNF145-triggered degradation of the lipid hydrolase ADIPOR2 [ EMBO J, 2022, 41-19:e110777] | PubMed: 35993436 |
Multiple Components of Protein Homeostasis Pathway Can Be Targeted to Produce Drug Synergies with VCP Inhibitors in Ovarian Cancer [ Cancers (Basel), 2022, 14(12)2949] | PubMed: 35740614 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.