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Aloxistatin

🥰Excellent
Catalog No. T6040Cas No. 88321-09-9
Alias Loxistatin, E64d, E64c ethyl ester

Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.

Aloxistatin

Aloxistatin

🥰Excellent
Purity: 99.47%
Catalog No. T6040Alias Loxistatin, E64d, E64c ethyl esterCas No. 88321-09-9
Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.
Pack SizePriceAvailabilityQuantity
1 mg$36In Stock
2 mg$51In Stock
5 mg$80In Stock
10 mg$122In Stock
25 mg$198In Stock
50 mg$369In Stock
100 mg$549In Stock
500 mg$1,190In Stock
1 mL x 10 mM (in DMSO)$64In Stock
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Purity:99.47%
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Product Introduction

Bioactivity
Description
Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.
In vitro
Aloxistatin can enter the intact platelet and inhibit proteolysis by inhibiting calpain. [2] Aloxistatin blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. [3]
In vivo
Aloxistatin (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. [1] In spinal cord injury (SCI) rats, Aloxistatin provides neuroprotection in SCI lesion and penumbra. [4] Aloxistatin reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. [5]
Kinase Assay
The CTLs and NK cells (0.8×106/mL) are treated with the inhibitors L1 (10-20 μM) or Aloxistatin (20-30 μM) for 24 hr at 37°C in 24-well plates. Cells are then used in 51Cr-release assays or are lysed to examine perforin in Western blots. The inhibitor is also added at the same concentration during the 4 hr reactions in some 51Cr-release assays, as indicated. Cell lysates are prepared using NP-40 lysis buffer (25 mM HEPES, 250 mM NaCl, 2.5 mM ethylenediaminetetraacetic acid, 0.1% volume/volume Nonidet P-40) and total protein concentration is determined using the Bradford assay. Equal amounts of protein are loaded and resolved on 8% SDS-PAGE gels. Human or mouse perforin is detected using the appropriate antibodies as indicated. Anti-actin antibody is used as a loading control[2].
Cell Research
Aloxistatin (E64d) is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.1 %) before use[3]. Cell proliferation and apoptosis are assessed by staining for a proliferation marker, Ki67, or an apoptotic marker, cleaved caspase 3, following the protocol described above for the polarity markers. MCF10 variants are grown in 3D rBM overlay cultures for 4 days and are treated with 0.1 % DMSO, 5 μM CA074Me or 5 μM Aloxistatin. The percentage of structures that are positive for Ki67 or cleaved caspase 3 is determined by counting a total of 100 structures on two separate coverslips with a Zeiss Axiophot epifluorescent microscope. Structures are considered Ki67 positive if they contained at least one cell staining for Ki67. Structures are considered to be caspase 3 positive if they contained at least one cell that is positive for cleaved caspase 3 and the positive cell(s) is not localized in the center of a developing lumen[3].
AliasLoxistatin, E64d, E64c ethyl ester
Chemical Properties
Molecular Weight342.43
FormulaC17H30N2O5
Cas No.88321-09-9
SmilesCCOC(=O)[C@H]1O[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)NCCC(C)C
Relative Density.1.0657 g/cm3 (Estimated)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (160.62 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9203 mL14.6015 mL29.2030 mL146.0152 mL
5 mM0.5841 mL2.9203 mL5.8406 mL29.2030 mL
10 mM0.2920 mL1.4602 mL2.9203 mL14.6015 mL
20 mM0.1460 mL0.7301 mL1.4602 mL7.3008 mL
50 mM0.0584 mL0.2920 mL0.5841 mL2.9203 mL
100 mM0.0292 mL0.1460 mL0.2920 mL1.4602 mL

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