MSC1094308 binding to drugable hotspot of p97 has the ability to block the D2 ATPase activity.[1]
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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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