Name: E 64d
Price: 306.00 USD

- Overview
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    Background
    
    E-64d, a membrane permeant derivative of E-64c, a thiol protease inhibitor1, was tested for ability to inhibit calpain activity in intact platelets.
    E-64c or E-64d also inhibited (lanes 3-8), demonstrating their effect on calpain. When the platelets were incubated with these inhibitors for I0 min and were then washed to remove extracellular inhibitor before lysis, neither E-64c nor leupeptin inhibited proteolysis, but E-64d did inhibit. E-64d was able to penetrate the platelet and was thus not removed by washing.E-64c failed to inhibit proteolysis in intact platelets, but E-64d, the permeant inhibitor, did inhibit intracellular proteolysis.E-64c and E-64d were each able to inhibit the protease activity in lysed platelets. This protease activity has been attributed to calpain by its absolute dependence on Ca 2+and by inhibition by known inhibitors of calpain. E-64d is able to enter the intact platelet: i) after washing to remove extracellular inhibitor, there was no protease activity detected after platelet lysis, and ii) activation of platelets preincubated with E-64d, but not E-64c, resulted in inhibition of proteolysis by calpain activated in intact platelets by A23187 plus calcium.
- Properties
  - Alternative Name
    
    ethyl (2S,3S)-3-[[(2S)-4-methyl-1-(3-methylbutylamino)-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylate
    
    CAS Number
    
    88321-09-9
    
    Molecular Formula
    
    C17H30N2O5
    
    Molecular Weight
    
    342.43
    
    Appearance
    
    A solid
    
    Purity
    
    98.17%
    
    Solubility
    
    insoluble in H2O; ≥17.12 mg/mL in DMSO; ≥18.5 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Cliff J. Luke, Stephanie Markovina, et al. "Lysoptosis is an evolutionarily conserved cell death pathway moderated by intracellular serpins." Commun Biol. 2022 Jan 12;5(1):47. PMID:35022507
    2. Jianhui Nie, Qianqian Li, et al. "Functional comparison of SARS-CoV-2 with closely related pangolin and bat coronaviruses." Cell Discov. 2021 Apr 6;7(1):21. PMID:33824288
    3. Wang LJ, Chiou JT, et al. "SIRT3, PP2A and TTP protein stability in the presence of TNF-α on vincristine-induced apoptosis of leukaemia cells." J Cell Mol Med. 2020;24(4):2552–2565. PMID:31930676
    4. Dziekan, Jerzy Michal. "Molecular analysis of antimalarial therapies : from drug development to mode of action." Nanyang Technological University. 2019.
    5. Maxine Bauzon, Penelope M. Drake, et al. "Maytansine-bearing antibody-drug conjugates induce in vitro hallmarks of immunogenic cell death selectively in antigen-positive target cells." OncoImmunology.Received 09 Aug 2018, Accepted 12 Dec 2018, Published online: 22 Jan 2019.
    6. An H, Harper JW. "Systematic analysis of ribophagy in human cells reveals bystander flux during selective autophagy." Nat Cell Biol. 2017 Dec 11. PMID:29230017
    7. Tsai YC, Kotiya A, et al. "Deubiquitinating enzyme VCIP135 dictates the duration of botulinum neurotoxin type A intoxication." Proc Natl Acad Sci U S A. 2017 Jun 27;114(26):E5158-E5166. PMID:28584101

E 64d

E 64d

Background

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