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AdipoGen Life Sciences
Aloxistatin [E-64d]
40
CHF
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
| 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
- 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)
- Thiol protease-specific inhibitor E-64 arrests human epidermoid carcinoma A431 cells at mitotic metaphase: Y. Shoji, et al.; PNAS 85, 146 (1988)
- 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)
- Inhibition of cysteine proteinases in lysosomes and whole cells: D. Wilcox & R.W. Mason; Biochem. J. 285, 495 (1992)
- 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)
- Neurovascular and neuronal protection by E64d after focal cerebral ischemia in rats: T. Tsubokawa, et al.; J. Neurosci. Res. 84, 832 (2006)
- Inhibition of Plasmodium falciparum oocyst production by membrane-permeant cysteine protease inhibitor E64d: S. Eksi, et al.; Antimicrob. Agents Chemother. 51, 1064 (2007)
- 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)
- Spatiotemporal organisation of protein processing in the kidney: M. Polesel, et al.; Nature Commun. 13, 5732 (2022)
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