SML1128
NMS-873
≥98% (HPLC), VCP/p97 inhibitor, powder
别名:
3- [3-环戊基磺酰基-5-（4′-甲磺酰基-2-甲基联苯基-4-氧基甲基）- [1,2,4] 三唑-4-基 ]-吡啶, 3- [3-（环戊基硫代）-5- [ [2-甲基-4′-（甲磺酰基） [1,1′-联苯基 ]-4-基 ] 氧 ] 甲基 ]-4H-1,2,4-三唑-4-基 ]-吡啶
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关于此项目
经验公式（希尔记法）:
C27H28N4O3S2
化学文摘社编号:
分子量:
520.67
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
NMS-873, ≥98% (HPLC)
SMILES string
CC1=CC(OCC2=NN=C(SC3CCCC3)N2C4=CN=CC=C4)=CC=C1C5=CC=C(S(C)(=O)=O)C=C5
InChI
1S/C27H28N4O3S2/c1-19-16-22(11-14-25(19)20-9-12-24(13-10-20)36(2,32)33)34-18-26-29-30-27(35-23-7-3-4-8-23)31(26)21-6-5-15-28-17-21/h5-6,9-17,23H,3-4,7-8,18H2,1-2H3
InChI key
UJGTUKMAJVCBIS-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 25 mg/mL, clear
storage temp.
2-8°C
Quality Level
Application
MS-873已被用作含三磷酸腺苷酶的蛋白质 (VCP)/p97 的变构抑制剂。
Biochem/physiol Actions
NMS-873 是 AAA ATP 酶家族成员缬氨酸包含蛋白 (VCP) 的选择性变构非 ATP 竞争性抑制剂，也称为 p97 (VCP/p97)。
NMS-873 是 AAA ATP 酶家族成员缬氨酸包含蛋白 (VCP) 的选择性变构非 ATP 竞争性抑制剂，也被称为 p97 (VCP/p97)，是泛素融合降解 (UFD) 途径的一个组成部分。VCP/p97 在降解错误折叠蛋白、高尔基体膜重组、膜转运、肌原纤维组装、自噬体成熟和细胞分裂中起作用，在许多肿瘤类型中过表达。NMS-873 是目前为止最强效和特异性 VCP 抑制剂。NMS-873 对 VCP/p97 的 IC 50 为 30 NM，而 IC 50 > 10μM 对抗所有 AAA atp 酶、HSP90 或分析的 53 种激酶。NMS-873 抑制 HCT116 癌细胞系细胞的增殖，IC 50 值为 400 NM。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Mike Blueggel et al.
Nature communications, 14(1), 3258-3258 (2023-06-06)
The AAA+ ATPase p97/VCP together with different sets of substrate-delivery adapters and accessory cofactor proteins unfolds ubiquitinated substrates to facilitate degradation by the proteasome. The UBXD1 cofactor is connected to p97-associated multisystem proteinopathy but its biochemical function and structural organization
Sahradha Albert et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(2), 1069-1080 (2019-12-29)
To promote the biochemical reactions of life, cells can compartmentalize molecular interaction partners together within separated non-membrane-bound regions. It is unknown whether this strategy is used to facilitate protein degradation at specific locations within the cell. Leveraging in situ cryo-electron
Replication-dependent unhooking of DNA interstrand cross-links by the NEIL3 glycosylase.
Semlow D R, et al.
Cell, 167(2), 498-511 (2016)
Claire Chavarria et al.
iScience, 26(10), 107777-107777 (2023-09-18)
The transcription factor NRF1 resides in the endoplasmic reticulum (ER) and is constantly transported to the cytosol for proteasomal degradation. However, when the proteasome is defective, NRF1 escapes degradation and undergoes proteolytic cleavage by the protease DDI2, generating a transcriptionally
Tycho E T Mevissen et al.
Cell reports, 42(2), 112125-112125 (2023-02-23)
Tripartite motif-containing protein 21 (TRIM21) is a cytosolic antibody receptor and E3 ubiquitin ligase that promotes destruction of a broad range of pathogens. TRIM21 also underlies the antibody-dependent protein targeting method Trim-Away. Current evidence suggests that TRIM21 binding to antibodies
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