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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 25 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
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 密鑰
UJGTUKMAJVCBIS-UHFFFAOYSA-N
應用
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。
生化／生理作用
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。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
其他客户在看
Mike Blueggel et al.
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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
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