Aloxistatin [E-64d]
| Code | Size | Price |
|---|
| PSI-11-077-5mg | 5mg | £356.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
blue ice or RT
Storage:
Short Term Storage: +4C. Long Term Storage: -20C. Handling Advice: Keep cool and dry. Use/Stability: Stable for at least 2 years after receipt when stored at -20C.
Documents
Further Information
Additional Names:
E-64c ethyl ester; EP 453; EST; Loxistatin
Background:
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).
CAS:
88321-09-9
Formula:
C17H30N2O5
Identity:
Determined by 1H-NMR.
InChi Key:
SRVFFFJZQVENJC-IHRRRGAJSA-N
Physical State:
Lyophilized
Predicted Molecular Weight:
342.4
Purity:
greater than or equal to 95% (HPLC)
Rtecs:
RR0404300
Smiles:
O=C(OCC)[C@H]1O[C@@H]1C(N[C@H](C(NCCC(C)C)=O)CC(C)C)=O
Solubility:
Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (5mg/ml).
Soluble In Dmf, Ethanol, Dmso Or Aqueous Solvents (Pbs).:
Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (5mg/ml).