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NFAT Inhibitor-1

  Cat. No.:  DC12660   Featured
Chemical Structure
249537-73-3
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Field of application
NFAT inhibitor is a cell-permeable compound that selectively inhibits calcineurin-mediated dephosphorylation of NFAT.
Cas No.: 249537-73-3
Chemical Name: NFAT Inhibitor-1
Synonyms: L-Glutamic acid,L-methionyl-L-alanylglycyl-L-prolyl-L-histidyl-L-prolyl-L-valyl-L-isoleucyl-L-valyl-L-isoleucyl-L-threonylglycyl-L-prolyl-L-histidyl-L-a-glutamyl-;L-Glutamic acid,L-methionyl-L-alanylglycyl-L-prolyl-L-histidyl-L-prolyl-L-valyl-L-isoleucyl-L-valyl-L-isoleucyl-L-threonylgly;NFAT Inhibitor;H-MET-ALA-GLY-PRO-HIS-PRO-VAL-ILE-VAL-ILE-THR-GLY-PRO-HIS-GLU-GLU-OH;MAGPHPVIVITGPHEE;MET-ALA-GLY-PRO-HIS-PRO-VAL-ILE-VAL-ILE-THR-GLY-PRO-HIS-GLU-GLU;VIVIT peptide;VIVIT;(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propano;NFAT Inhibitor-1
SMILES: S(C)CC[C@@H](C(N([H])[C@@H](C)C(N([H])CC(N1CCC[C@H]1C(N([H])[C@@H](CC1=CN=CN1[H])C(N1CCC[C@H]1C(N([H])[C@H](C(N([H])[C@H](C(N([H])[C@H](C(N([H])[C@H](C(N([H])[C@@H]([C@@H](C)O)C(N([H])CC(N1CCC[C@H]1C(N([H])[C@H](C(N([H])[C@H](C(N([H])[C@H](C(=O)O)CCC(=O)O)=O)CCC(=O)O)=O)CC1=CN=CN1[H])=O)=O)=O)=O)[C@@H](C)CC)=O)C(C)C)=O)[C@@H](C)CC)=O)C(C)C)=O)=O)=O)=O)=O)=O)N([H])[H]
Formula: C75H118N20O22S
M.Wt: 1683.92523622513
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Does not disrupt other calcineurin-dependent pathways. Inhibits NFAT activation and NFAT-dependent expression of endogenous cytokine genes in T cells.
In Vitro: NFAT Inhibitor (VIVIT peptide) is superior at inhibiting calcineurin-mediated dephosphorylation of NFAT1, NFAT2, and NFAT4 in cell extracts. NFAT Inhibitor (100 μM) that effectively inhibits NFAT1-calcineurin binding and NFAT1 dephosphorylation, does not inhibit calcineurin phosphatase activity toward the RII phosphopeptide. NFAT Inhibitor selectively inhibits NFAT activation without disrupting other calcineurin-dependent pathways[1]. NFAT Inhibitor attenuates NFAT-dependant protein expression in immune cells. NFAT activity regulates proinflammatory secretion and is attenuated by NFAT Inhibitor in murine microglia cultures[2].
References: [1]. Aramburu J, et al. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999 Sep 24;285(5436):2129-33. [2]. Nagamoto-Combs K, et al. Microglial phenotype is regulated by activity of the transcription factor, NFAT (nuclear factor of activated T cells). J Neurosci. 2010 Jul 14;30(28):9641-6.
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