400-998-5282
专注多肽 服务科研
400-998-5282
专注多肽 服务科研
一种 NFAT 的细胞渗透性肽抑制剂，可选择性抑制钙调磷酸酶介导的 NFAT 脱磷酸作用。
编号：131865
CAS号：249537-73-3
单字母：H2N-MAGPHPVIVITGPHEE-OH
| 参考文献（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) . <ALLPEPTIDE>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) . <ALLPEPTIDE>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) . |
| 溶解度: | DMSO: 15 mg/ml Water: 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/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 |
| 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-glutamicacid |
NFAT Inhibitor (VIVIT peptide) 是一种 NFAT 的细胞渗透性肽抑制剂，可选择性抑制钙调磷酸酶介导的 NFAT 脱磷酸作用。
NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT[1][2].
活化 T 细胞核因子抑制肽是靶向该转录因子的多肽抑制剂，结合钙调磷酸酶上识别位点，不影响其磷酸酶活性，呈浓度依赖性抑制活化 T 细胞核因子去磷酸化，可抑制多种细胞内该转录因子激活。
NFAT inhibitor is a peptide inhibitor of the transcription factor nuclear factor of activated T cells (NFAT). It binds to the NFAT recognition site on the protein phosphatase calcineurin (IC = 25 pM) but does not inhibit calcineurin phosphatase activity when used at a concentration of 100 µM. NFAT inhibitor inhibits the dephosphorylation of NFAT in HEK293T lysates expressing NFAT1, -2, or -4 in a concentration-dependent manner. It inhibits NFAT activation in RAW 264.7 macrophages, EA.hy926 endothelial cells, and isolated mouse thoracic aorta vascular smooth muscle cells (VSMCs; IC s = 29.1, 30.2, and 45.7 µM, respectively, in reporter assays).
| DOI | 名称 | |
|---|---|---|
| 10.1126/science.285.5436.2129 | Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A | 下载 |
| 10.1002/art.40868 | Activation of the Peroxisome Proliferator-Activated Receptor γ Coactivator 1β/NFATc1 Pathway in Circulating Osteoclast Precursors Associated With Bone Destruction in Rheumatoid Arthritis | 下载 |
