AEBSF . hydrochloride (CAS: 30827-99-7)

C₈H₁₀FNO₂S . HCl

• Water soluble, irreversible serine protease (chymotrypsin, kallikrein, plasmin, thrombin and trypsin) inhibitor. Stable, non-toxic alternative to PMSF.
• Potent, selective inhibitor of Site-1-protease (S1P).
• Used to characterize the downstream result of SREBP inhibition and its influence on cholesterol regulation by selectively inhibiting S1P.
• NAD(P)H oxidase inhibitor.
• Inhibits activation of TGFβ and activates JNK and p38 MAP kinases.
• β-Secretase inhibitor. Shown to inhibit β-amyloid peptide production and enhance APP (amyloid precursor protein) secretion in several cell lines at millimolar concentrations.

1. Irreversible enzyme inhibitors. 180. Irreversible inhibitors of the Cla component of complement derived from m-(phenoxypropoxy)benzamidine and phenoxyacetamide: B.R. Baker & M. Cory; J. Med. Chem. 14, 119 (1971)
2. Synthetic low molecular weight inhibitors of serum kallikrein: F. Markwardt, et al.; Biochem. Pharmacol. 23, 2247 (1974)
3. Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF: M. Citron, et al.; Neuron 17, 171 (1996)
4. Inhibition of NADPH oxidase activation by 4-(2-aminoethyl)-benzenesulfonyl fluoride and related compounds: V. Diatchuk, et al.; J. Biol. Chem. 272, 13292 (1997)
5. 4-(2-Aminoethyl)benzenesulfonyl fluoride attenuates tumor-necrosis-factor-alpha-induced blood-brain barrier opening: P. Megyeri, et al.; Eur. J. Pharmacol. 374, 207 (1999)
6. Irreversible inhibitors of serine, cysteine, and threonine proteases: J.C. Powers, et al.; Chem. Rev. 102, 4639 (2002)
7. A serine protease inhibitor prevents endoplasmic reticulum stress-induced cleavage but not transport of the membrane-bound transcription factor ATF6: T. Okada, et al.; J. Biol. Chem. 278, 31024 (2003)
8. Proteolytic activation of latent TGF-beta precedes caspase-3 activation and enhances apoptotic death of lung epithelial cells: V.T. Solovyan & J. Keski-Oja; J. Cell Physiol. 207, 445 (2006)
9. Serine protease inhibitor attenuates ovalbumin induced inflammation in mouse model of allergic airway disease: S. Saw, et al.; PLoS One 7, e41107 (2012)