a quinazolin compound that acts as a specific and potent inhibitor of autophagy
Synonym(s):
Spautin-1, Autophagy Inhibitor II, C43, 6-fluoro-N-[4-fluorobenzyl]quinazolin-4-amine, Specific and Potent AUtophagy Inhibitor 1, C43, 6-fluoro-N-[4-fluorobenzyl]quinazolin-4-amine, Specific and Potent AUtophagy Inhibitor 1, Autophagy Inhibitor II
A quinazolin compound that acts as a specific and potent inhibitor of autophagy and promotes Vps34 PI 3-kinase complex degradation by blocking the activity of USP 10 (IC50 = 580 nM) and USP 13 (IC50 = 690 nM) deubiquitinating enzymes. However, it does not affect the lipid kinase activity of Vps34. Also shown to reduce the level of cytoplasmic and nuclear p53. Sensitizes breast cancer cell lines (BCAP37, MCF-7, and BT549) to apoptosis under conditions of nutritional deprivation. Also shown to inhibit etoposide-induced cell death in Bax/Bak double knockout (DKO) cells. Normal cell lines (e.g., MDCK cells) do not undergo autophagy in the presence of Spautin-1.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lui, J., et al. 2011, Cell.147, 223.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Tauopathies are a collection of neurodegenerative diseases characterized by the accumulation of pathogenic aggregates of the microtubule-associated protein tau. Despite the prevalence and diversity of tau astrogliopathy in tauopathies, the interactions between astrocytes and tau in the brain, and the
Frontiers in pharmacology, 11, 580343-580343 (2020-11-13)
Macroautophagy (hereafter autophagy) is a multistep intracellular catabolic process with pleiotropic implications in cell fate. Attending to its activation, autophagy can be classified into inducible or constitutive. Constitutive, or basal autophagy, unfolds under nutrient-replete conditions to maintain the cellular homeostasis.
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