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Submit ReviewNMS 873 is a potent p97 ATPase (VCP) allosteric inhibitor (IC50 = 30 nM). Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 μM). Activates the unfolded protein response (UPR) and modulates autophagosome maturation. Exhibits antiproliferative activity in cancer cells in vitro (IC50 values are 400 and 700 nM for HCT116 and HeLa cells respectively). Reduces p97-sensitization to trypsin digestion.
NMS 873 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 520.67 |
公式 | C27H28N4O3S2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1418013-75-8 |
PubChem ID | 71521142 |
InChI Key | UJGTUKMAJVCBIS-UHFFFAOYSA-N |
Smiles | CC1=C(C2=CC=C(S(C)(=O)=O)C=C2)C=CC(OCC3=NN=C(N3C4=CN=CC=C4)SC5CCCC5)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 52.07 | 100 |
以下数据基于产品分子量 520.67。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.92 mL | 9.6 mL | 19.21 mL |
5 mM | 0.38 mL | 1.92 mL | 3.84 mL |
10 mM | 0.19 mL | 0.96 mL | 1.92 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
参考文献是支持产品生物活性的出版物。
Magnaghi et al (2013) Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. Nat.Chem.Biol. 9 548 PMID: 23892893
Anderson et al (2015) Targeting the AAA ATPase p97 as an approach to treat cancer through disruption of protein homeostasis. Cancer Cell 28 653 PMID: 26555175
Polucci et al (2013) Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. J.Med.Chem. 56 437 PMID: 23245311
If you know of a relevant reference for NMS 873, please let us know.
关键词: NMS 873, NMS 873 supplier, NMS873, Potent, selective, valosine, containing, protein, VCP, p97, allosteric, inhibitors, inhibits, unfolded, response, UPR, autophagosome, maturation, antiproliferative, anticancer, Autophagy, Other, ER, stress/UPR, ATPase, Translocation, 6180, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NMS 873 的部分引用包括:
Manu et al (2020) Protein translocation and retro-translocation across the endoplasmic reticulum are crucial to inflammatory effector CD4+ T cell function. Cytokine 129 154944 PMID: 32146280
Yong et al (2020) Tandem Deubiquitination and Acetylation of SPRTN Promotes DNA-Protein Crosslink Repair and Protects against Aging. Mol Cell 79 824-835.e5 PMID: 32649882
Oscar et al (2021) USP7 and VCPFAF1 define the SUMO/Ubiquitin landscape at the DNA replication fork. Cell Rep 37 109819 PMID: 34644576
Keith et al (2022) Compounds activating VCP D1 ATPase enhance both autophagic and proteasomal neurotoxic protein clearance. Nat Commun 13 4146 PMID: 35842429
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平均评分: 3 (Based on 1 Review.)
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This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.