AdipoGen Life Sciences

Aloxistatin [E-64d]

CHF 40.00
In stock
AG-CR1-3737-M0011 mgCHF 40.00
AG-CR1-3737-M0055 mgCHF 90.00
AG-CR1-3737-M02525 mgCHF 270.00
More Information
Product Details
Synonyms E-64c ethyl ester; EP 453; EST; Loxistatin
Product Type Chemical
Properties
Formula

C17H30N2O5

MW 342.4
CAS 88321-09-9
RTECS RR0404300
Purity Chemicals ≥95% (HPLC)
Appearance White to off-white powder.
Solubility Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (5mg/ml).
Identity Determined by 1H-NMR.
InChi Key SRVFFFJZQVENJC-IHRRRGAJSA-N
Smiles O=C(OCC)[C@H]1O[C@@H]1C(N[C@H](C(NCCC(C)C)=O)CC(C)C)=O
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Keep under inert gas.
Protect from moisture and oxygen.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Description
  • Aloxistatin [E-64d] is a cell permeable irreversible inhibitor of lysosomal and cytosolic cysteine proteases cathepsin B an L, calpain 1/2, papain and has diverse biological activities. It is an ethyl ester form of E-64c that inhibits calpain and the cysteine proteases cathepsins F, K, B, H, and L.
  • Aloxistatin has anticancer properties by inducing cell cycle arret at the G2/M phase in A431 human epidermoid carcinoma cells and as a lysosomal inhibitor in human acute promyelocytic leukemia NB4 cells and Huh-7 cells. It inhibits degradation of autophagic cargo inside autolysosomes.
  • It also shows neuroprotective and anti-malarial properties.
  • Since cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, aloxistatin treatment reduces cellular entry of SARS-CoV-2 pseudovirions and COVID-19. It inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) and SARS-CoV-2 surface glycoprotein incorporation into pseudotyped vesicular stomatitis virus (VSV) particles in Vero cells. Is has been applied in vitro in combination with the TMPRSS2 inhibitor camostat mesylate (Prod. No. AG-CR1-3716).
Product References
  1. In vitro and in vivo inhibition of cysteine proteinases by EST, a new analog of E-64: M. Tamai, et al.; J. Pharmacobiodyn. 9, 672 (1986)
  2. Thiol protease-specific inhibitor E-64 arrests human epidermoid carcinoma A431 cells at mitotic metaphase: Y. Shoji, et al.; PNAS 85, 146 (1988)
  3. Inhibition of Calpain in intact platelets by the thiol protease inhibitor E-64d: E.B. McGowan, et al.; Biochem. Biophys. Res. Commun. 158, 432 (1989)
  4. Inhibition of cysteine proteinases in lysosomes and whole cells: D. Wilcox & R.W. Mason; Biochem. J. 285, 495 (1992)
  5. Increased calpain expression is associated with apoptosis in rat spinal cord injury: calpain inhibitor provides neuroprotection: S.K. Ray, et al.; Neurochem. Res. 25, 1191 (2000)
  6. Neurovascular and neuronal protection by E64d after focal cerebral ischemia in rats: T. Tsubokawa, et al.; J. Neurosci. Res. 84, 832 (2006)
  7. Inhibition of Plasmodium falciparum oocyst production by membrane-permeant cysteine protease inhibitor E64d: S. Eksi, et al.; Antimicrob. Agents Chemother. 51, 1064 (2007)
  8. SARS-CoV-2 cell entry depends on ACE2 and TMPRSS2 and is blocked by a clinically proven protease inhibitor: M. Hoffmann, et al.; Cell 181, 271 (2020)
  9. Spatiotemporal organisation of protein processing in the kidney: M. Polesel, et al.; Nature Commun. 13, 5732 (2022)
© 2017 Adipogen Life Sciences. Pictures: © 2012 Martin Oeggerli. All Rights Reserved.