SML2326
MSC1094308
≥98% (HPLC)
别名:
N-((6-Fluoro-2,3,4,9-tetrahydro-1H-carbazol-3-yl)methyl)-4,4-bis(4-fluorophenyl)butan-1-amine, N-[4,4-Bis(4-fluorophenyl)butyl]-6-fluoro-2,3,4,9-tetrahydro-1H-carbazole-3-methanamine
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
FC1=CC=C(C(C2=CC=C(F)C=C2)CCCNCC3CCC(NC4=C5C=C(F)C=C4)=C5C3)C=C1
InChI key
OCZIMUMAPGQEBH-UHFFFAOYSA-N
相关类别
生化/生理作用
MSC1094308 binding to drugable hotspot of p97 has the ability to block the D2 ATPase activity.
MSC1094308 is a reversible, non-ATP-competitive, type I AAA ATPase VPS4B-selective allosteric inhibitor (IC50 = 0.71 μM) with =10-fold reduced potency toward the type II AAA ATPase VCP/p97 and NSF (IC50 = 7.2 and >40 μM, respectively). MSC1094308 specifically inhibits p97-mediated Ub-GFP degradation without affecting proteasome-dependent ODD-luc degradation using a dual reporter HeLa cell line (10 μM) and exhibits comparable efficacy as DBeQ against 50 ng/mL TNFα-induced IκBα degradation in HeLa cells (10 μM).
Reversible, non-ATP-competitive, AAA ATPase VPS4B & VCP/p97 allosteric inhibitor against cellular p97, but not proteasome, substrates degradation.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Robert Pöhler et al.
Angewandte Chemie (International ed. in English), 57(6), 1576-1580 (2017-12-23)
AAA ATPases have pivotal functions in diverse cellular processes essential for survival and proliferation. Revealing strategies for chemical inhibition of this class of enzymes is therefore of great interest for the development of novel chemotherapies or chemical tools. Here, we
A Non-Competitive Inhibitor of VCP/p97 and VPS4 Reveals Conserved Allosteric Circuits in Type I and II AAA ATPases
Pohler R, et al.
Angewandte Chemie (International Edition in English), 57(6), 1576-1580 (2018)
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