A peptide inhibitor of NFAT
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NFAT Inhibitor

Item No. 13855

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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-α-glutamyl-L-glutamic acid
CAS Number
249537-73-3
Synonyms
  • Nuclear Factor of Activated T cells Inhibitor
  • VIVIT
Molecular Formula
C75H118N20O22S
Formula Weight
1683.9
Purity
≥95%
Formulation (Request formulation change)
A lyophilized powder
Solubility(Learn about Variance in Solubility)
DMSO: 15 mg/mlWater: 10 mg/ml
SMILES
O=C(N(CCC1)[C@@H]1C(N[C@@H](C(C)C)C(N[C@]([C@@H](C)CC)([H])C(N[C@@H](C(C)C)C(N[C@]([C@@H](C)CC)([H])C(N[C@]([C@H](O)C)([H])C(NCC(N(CCC2)[C@@H]2C(N[C@H](C(N[C@@H](CCC(O)=O)C(N[C@H](C(O)=O)CCC(O)=O)=O)=O)CC3=CNC=N3)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC4=CNC=N4)NC([C@H](CCC5)N5C(CNC([C@H](C)NC([C@@H](N)CCSC)=O)=O)=O)=O
InChi Code
InChI=1S/C75H118N20O22S/c1-12-39(7)59(90-70(111)57(37(3)4)88-68(109)52-19-16-27-95(52)74(115)49(30-44-32-78-36-82-44)87-67(108)51-18-15-26-94(51)53(97)33-79-62(103)41(9)83-63(104)45(76)24-28-118-11)72(113)89-58(38(5)6)71(112)91-60(40(8)13-2)73(114)92-61(42(10)96)69(110)80-34-54(98)93-25-14-17-50(93)66(107)86-48(29-43-31-77-35-81-43)65(106)84-46(20-22-55(99)100)64(105)85-47(75(116)117)21-23-56(101)102/h31-32,35-42,45-52,57-61,96H,12-30,33-34,76H2,1-11H3,(H,77,81)(H,78,82)(H,79,103)(H,80,110)(H,83,104)(H,84,106)(H,85,105)(H,86,107)(H,87,108)(H,88,109)(H,89,113)(H,90,111)(H,91,112)(H,92,114)(H,99,100)(H,101,102)(H,116,117)/t39-,40-,41-,42+,45-,46-,47-,48-,49-,50-,51-,52-,57-,58-,59-,60-,61-/m0/s1
InChi Key
QPMHUXBSHGAVGD-MCDIZDEASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NFAT inhibitor is a peptide inhibitor of the transcription factor nuclear factor of activated T cells (NFAT).1 It binds to the NFAT recognition site on the protein phosphatase calcineurin (IC50 = 25 pM) but does not inhibit calcineurin phosphatase activity when used at a concentration of 100 µM.2,1 NFAT inhibitor inhibits the dephosphorylation of NFAT in HEK293T lysates expressing NFAT1, -2, or -4 in a concentration-dependent manner.1 It inhibits NFAT activation in RAW 264.7 macrophages, EA.hy926 endothelial cells, and isolated mouse thoracic aorta vascular smooth muscle cells (VSMCs; IC50s = 29.1, 30.2, and 45.7 µM, respectively, in reporter assays).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aramburu, J., Yaffe, M.B., López-Rodríguez, C., et al. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science 285(5436), 2129-2133 (1999).

    2. Roehrl, M.H.A., Kang, S., Aramburu, J., et al. Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules. Proc. Natl. Acad. Sci. USA 101(20), 7554-7559 (2004).

    3. Yu, H., Sliedregt-Bol, K., Overkleeft, H., et al. Therapeutic potential of a synthetic peptide inhibitor of nuclear factor of activated T cells as antirestenotic agent. Arterioscler. Thromb. Vasc. Biol. 26(7), 1531-1537 (2006).

    Product Citations

    Zhao, X., Guo, Y., Jiang, C., et al. JNK1 negatively controls antifungal innate immunity by suppressing CD23 expression. Nat. Med. 23(3), 337-346 (2017).