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Chemical Compound Review

N-Allm     (2S)-2-[[(2S)-2-acetamido-4- methyl...

Synonyms: CHEMBL318779, Cpi(2), AC1L3TIY, ZINC03874336, LS-172109, ...
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Disease relevance of Ac-Leu-Leu-Met-H


High impact information on Ac-Leu-Leu-Met-H


Biological context of Ac-Leu-Leu-Met-H


Anatomical context of Ac-Leu-Leu-Met-H

  • Calpain inhibitor 2 prevents axonal degeneration of opossum optic nerve fibers [14].
  • Calpain inhibitor 2, administered 10 min after injury via continuous arterial infusion into the right external carotid artery for 24 h, significantly reduced neurofilament 200 losses to 17% and 3% relative to naive neurofilament 200 protein levels in the ipsilateral and contralateral cortices, respectively [2].
  • Accordingly, we investigated the effects of lactacystin, a proteasome inhibitor, and calpain inhibitor-II (CI-II) on L8 muscle cell differentiation and assessed concentrations of proteasomal and calpain subunit mRNAs during differentiation [15].
  • We show that the extracellular application of two newly developed, highly potent calpain inhibitors, N-acetyl-Leu-Leu-norleucinal and N-acetyl-Leu-Leu-methioninal, block LTP in both the Schaffer collateral-CA1 synaptic zone of the rat hippocampal slice and in perforant path-stimulated dentate granule cells in the intact hippocampus [16].

Associations of Ac-Leu-Leu-Met-H with other chemical compounds


Gene context of Ac-Leu-Leu-Met-H

  • When m-calpain activity and myoblast fusion were prevented by addition of antibodies to m-calpain or calpain inhibitor II, the fibronectin concentration was higher since it was increased by approximately 67 and approximately 71%, respectively [21].
  • Calpain inhibitor II (N-acetyl-Leu-Leu-methionyl) provided protection only with a narrow dose range, whereas carbobenzoxy-Asp-CH2-OC(O)-2,6-dichlorobenzene (Z-D-DCB; pan-caspase inhibitor) and MK-801 (N-methyl-D-aspartate receptor antagonist) were potently effective across a wider dose range [22].
  • Calpain inhibitors E64d (100 microM) and calpain inhibitor II (1 mM) were ineffective in preventing opacity formation caused by DCVC [23].
  • Staurosporine-induced loss of neuronal particles was blocked by nonselective caspase inhibition (z-VAD-fmk) and by calpain inhibition (calpain inhibitor II [ALLM]) [24].
  • Moreover, protease inhibitors fail to abrogate CD95 ligand-induced apoptosis even though DNA fragmentation is attenuated by calpain inhibitor II and TPCK [25].


  1. Calpain inhibitor II induces caspase-dependent apoptosis in human acute lymphoblastic leukemia and non-Hodgkin's lymphoma cells as well as some solid tumor cells. Zhu, D.M., Uckun, F.M. Clin. Cancer Res. (2000) [Pubmed]
  2. A calpain inhibitor attenuates cortical cytoskeletal protein loss after experimental traumatic brain injury in the rat. Posmantur, R., Kampfl, A., Siman, R., Liu, J., Zhao, X., Clifton, G.L., Hayes, R.L. Neuroscience (1997) [Pubmed]
  3. Systemic administration of a calpain inhibitor reduces behavioral deficits and blood-brain barrier permeability changes after experimental subarachnoid hemorrhage in the rat. Germanò, A., Costa, C., DeFord, S.M., Angileri, F.F., Arcadi, F., Pike, B.R., Bramanti, P., Bausano, B., Zhao, X., Day, A.L., Anderson, D.K., Hayes, R.L. J. Neurotrauma (2002) [Pubmed]
  4. Moderate hypothermia, but not calpain inhibitor 2, attenuates the proteolysis of microtubule-associated protein 2 in the hippocampus following traumatic brain injury in rats. Haranishi, Y., Kawata, R., Fukuda, S., Kiyoshima, T., Morimoto, Y., Matsumoto, M., Sakabe, T. European journal of anaesthesiology. (2005) [Pubmed]
  5. Effect of cold preservation on intracellular calcium concentration and calpain activity in rat sinusoidal endothelial cells. Upadhya, G.A., Topp, S.A., Hotchkiss, R.S., Anagli, J., Strasberg, S.M. Hepatology (2003) [Pubmed]
  6. Activation of the heat shock factor 1 by serine protease inhibitors. An effect associated with nuclear factor-kappaB inhibition. Rossi, A., Elia, G., Santoro, M.G. J. Biol. Chem. (1998) [Pubmed]
  7. Proteolytic regulation of the zinc finger transcription factor YY1, a repressor of muscle-restricted gene expression. Walowitz, J.L., Bradley, M.E., Chen, S., Lee, T. J. Biol. Chem. (1998) [Pubmed]
  8. Calcium/calmodulin-dependent protein kinase IV is cleaved by caspase-3 and calpain in SH-SY5Y human neuroblastoma cells undergoing apoptosis. McGinnis, K.M., Whitton, M.M., Gnegy, M.E., Wang, K.K. J. Biol. Chem. (1998) [Pubmed]
  9. Downregulation of IRS-1 protein in thapsigargin-treated human prostate epithelial cells. Zhang, H., Hoff, H., Sell, C. Exp. Cell Res. (2003) [Pubmed]
  10. Temporal relationships between de novo protein synthesis, calpain and caspase 3-like protease activation, and DNA fragmentation during apoptosis in septo-hippocampal cultures. Pike, B.R., Zhao, X., Newcomb, J.K., Wang, K.K., Posmantur, R.M., Hayes, R.L. J. Neurosci. Res. (1998) [Pubmed]
  11. Detailed analysis of cell cycle kinetics upon proteasome inhibition. Machiels, B.M., Henfling, M.E., Gerards, W.L., Broers, J.L., Bloemendal, H., Ramaekers, F.C., Schutte, B. Cytometry. (1997) [Pubmed]
  12. Maitotoxin induces calpain but not caspase-3 activation and necrotic cell death in primary septo-hippocampal cultures. Zhao, X., Pike, B.R., Newcomb, J.K., Wang, K.K., Posmantur, R.M., Hayes, R.L. Neurochem. Res. (1999) [Pubmed]
  13. Protein kinase C isoforms in muscle cells and their regulation by phorbol ester and calpain. Hong, D.H., Huan, J., Ou, B.R., Yeh, J.Y., Saido, T.C., Cheeke, P.R., Forsberg, N.E. Biochim. Biophys. Acta (1995) [Pubmed]
  14. Calpain inhibitor 2 prevents axonal degeneration of opossum optic nerve fibers. Araújo Couto, L., Sampaio Narciso, M., Hokoç, J.N., Blanco Martinez, A.M. J. Neurosci. Res. (2004) [Pubmed]
  15. Evidence for the participation of the proteasome and calpain in early phases of muscle cell differentiation. Ueda, Y., Wang, M.C., Ou, B.R., Huang, J., Elce, J., Tanaka, K., Ichihara, A., Forsberg, N.E. Int. J. Biochem. Cell Biol. (1998) [Pubmed]
  16. Calpain inhibitors block long-term potentiation. Denny, J.B., Polan-Curtain, J., Ghuman, A., Wayner, M.J., Armstrong, D.L. Brain Res. (1990) [Pubmed]
  17. Involvement of proteasomes in migration and matrix metalloproteinase-9 production of oral squamous cell carcinoma. Ikebe, T., Takeuchi, H., Jimi, E., Beppu, M., Shinohara, M., Shirasuna, K. Int. J. Cancer (1998) [Pubmed]
  18. Calpain and N-methyl-d-aspartate (NMDA)-induced excitotoxicity in rat retinas. Chiu, K., Lam, T.T., Ying Li, W.W., Caprioli, J., Kwong Kwong, J.M. Brain Res. (2005) [Pubmed]
  19. Calpain inhibitors protect auditory sensory cells from hypoxia and neurotrophin-withdrawal induced apoptosis. Cheng, A.G., Huang, T., Stracher, A., Kim, A., Liu, W., Malgrange, B., Lefebvre, P.P., Schulman, A., Van de Water, T.R. Brain Res. (1999) [Pubmed]
  20. Very low levels of methylmercury induce cell death of cultured rat cerebellar neurons via calpain activation. Sakaue, M., Okazaki, M., Hara, S. Toxicology (2005) [Pubmed]
  21. Myoblast fusion requires fibronectin degradation by exteriorized m-calpain. Dourdin, N., Brustis, J.J., Balcerzak, D., Elamrani, N., Poussard, S., Cottin, P., Ducastaing, A. Exp. Cell Res. (1997) [Pubmed]
  22. Novel characteristics of glutamate-induced cell death in primary septohippocampal cultures: relationship to calpain and caspase-3 protease activation. Zhao, X., Newcomb, J.K., Pike, B.R., Wang, K.K., d'Avella, D., Hayes, R.L. J. Cereb. Blood Flow Metab. (2000) [Pubmed]
  23. Mechanistic analysis of S-(1,2-dichlorovinyl)-L-cysteine-induced cataractogenesis in vitro. Walsh Clang, C.M., Aleo, M.D. Toxicol. Appl. Pharmacol. (1997) [Pubmed]
  24. Caspase inhibition protects nerve terminals from in vitro degradation. Gylys, K.H., Fein, J.A., Cole, G.M. Neurochem. Res. (2002) [Pubmed]
  25. Inhibition of drug-induced DNA fragmentation, but not cell death, of glioma cells by non-caspase protease inhibitors. Eitel, K., Wagenknecht, B., Weller, M. Cancer Lett. (1999) [Pubmed]
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