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Aloxistatin

Catalog No. T6040 CAS 88321-09-9

Synonyms: E64d, Loxistatin, 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.

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Aloxistatin, CAS 88321-09-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 36.00
2 mg	In stock	$ 51.00
5 mg	In stock	$ 80.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
500 mg	In stock	$ 1,190.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 99.47%

Purity: 99.46%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Synonyms	E64d, Loxistatin, E64c ethyl ester
Molecular Weight	342.43
Formula	C17H30N2O5
CAS No.	88321-09-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.9 mg/mL (20 mM)

References and Literature

1. Tamai M, et al. J Pharmacobiodyn. 1986, 9(8), 672-677. 2. McGowan EB, et al. Biochem Biophys Res Commun. 1989, 158(2), 432-435. 3. Murray EJ, et al. Metabolism. 1997 , 46(9), 1090-1094. 4. Ray SK, et al. Ann N Y Acad Sci. 2001, 939, 436-449. 5. Hook G, et al. J Alzheimers Dis. 2011, 26(2), 387-408.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Aging Compound Library ReFRAME Related Library Human Metabolite Library Anti-Infection Compound Library Covalent Inhibitor Library NO PAINS Compound Library Bioactive Compounds Library Max

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Keywords

Aloxistatin 88321-09-9 Microbiology/Virology Proteases/Proteasome Cysteine Protease SARS-CoV Cathepsin Inhibitor inhibit E64d Loxistatin E64c ethyl ester SARS coronavirus inhibitor

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