NFAT Inhibitor
(Synonyms: VIVIT peptide) 目录号 : GC17966
NFAT inhibitor是活化T细胞核因子（NFAT）的细胞渗透性肽抑制剂，选择性抑制钙调磷酸酶介导的NFAT的去磷酸化。
Cas No.:249537-73-3
Sample solution is provided at 25 µL, 10mM.
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NFAT Inhibitor is a cell-permeable peptide inhibitor of nuclear factor of activated T cells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT[1]. NFAT inhibitors inhibit the transcriptional activity of NFAT by directly binding to the NFAT protein and interfering with its binding to DNA, thereby affecting the expression of related genes[2]. The NFAT protein family plays a key role in immune responses, primarily regulating the transcription of cytokine genes and other genes that are important to immune responses[3][4]. NFAT Inhibitor is commonly used in immunology and cardiovascular-related research[5][6].
In vitro, NFAT inhibitor (1µM; 48h) significantly decreased NFAT-driven transcriptional activity and inhibited the expression of endogenous NFAT-target genes such as COX2, c-MYC, and CCND1 in LN229 glioma cells[7].
References:
[1] Aramburu J, Yaffe MB, López-Rodríguez C, Cantley LC, Hogan PG, Rao A. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999;285(5436):2129-2133.
[2] Ma JD, Jing J, Wang JW, et al. Activation of the Peroxisome Proliferator-Activated Receptor γ Coactivator 1β/NFATc1 Pathway in Circulating Osteoclast Precursors Associated With Bone Destruction in Rheumatoid Arthritis. Arthritis Rheumatol. 2019;71(8):1252-1264.
[3] Macian F. NFAT proteins: key regulators of T-cell development and function. Nat Rev Immunol. 2005;5(6):472-484.
[4] Martínez-Martínez S, Redondo JM. Inhibitors of the calcineurin/NFAT pathway. Curr Med Chem. 2004;11(8):997-1007.
[5] Yu H, van Berkel TJ, Biessen EA. Therapeutic potential of VIVIT, a selective peptide inhibitor of nuclear factor of activated T cells, in cardiovascular disorders. Cardiovasc Drug Rev. 2007;25(2):175-187.
[6] Samuelsson AM, Bayer AL, Li J, et al. Targeting of CIP4-Calcineurin Signalosomes Improves Cardiac Structure and Function After Myocardial Infarction. Preprint. bioRxiv. 2025;2025.05.12.653597.
[7] Ellert-Miklaszewska A, Szymczyk A, Poleszak K, Kaminska B. Delivery of the VIVIT Peptide to Human Glioma Cells to Interfere with Calcineurin-NFAT Signaling. Molecules. 2021;26(16):4785.
NFAT inhibitor是活化T细胞核因子（NFAT）的细胞渗透性肽抑制剂，选择性抑制钙调磷酸酶介导的NFAT的去磷酸化[1]。NFAT Inhibitor通过直接结合NFAT蛋白，干扰其与DNA的结合，从而抑制NFAT的转录活性，进而影响相关基因的表达[2]。NFAT蛋白家族在免疫反应中起着关键作用，主要调节细胞因子基因和其他对免疫反应至关重要的基因的转录[3][4]。NFAT Inhibitor通常用于免疫和心血管相关研究[5][6]。
在体外实验中，NFAT inhibitor（1μM；48小时）显著降低了LN229胶质瘤细胞中NFAT驱动的转录活性，并抑制了内源性NFAT靶基因（如COX2、c-MYC和CCND1）的表达[7]。
| Cell experiment []: | |
Cell lines | human glioma LN229 cells |
Preparation Method | Human glioma LN229 cells were grown in Dulbecco’s Modified Eagle’s Medium supplemented with 10% FBS and antibiotics (50U/mL penicillin, 50µg/mL streptomycin) under standard conditions. Cells were cultured in 96-well plates and treated with NFAT inhibitor (1µM) for 48h. The effects of the treatments were monitored at various time points by phasecontrast microscopy. Cells were collected for RT-PCR and Western Blot Analyses. |
Reaction Conditions | 1µM; 48h |
Applications | NFAT inhibitor (1µM; 48h) significantly inhibited the expression of endogenous NFAT-target genes such as COX2, c-MYC, and CCND1 in LN229 glioma cells. |
References: | |
| Cas No. | 249537-73-3 | SDF | |
| 别名 | VIVIT peptide | ||
| 化学名 | (S)-2-((Z)-((S)-2-((Z)-((S)-2-((Z)-(((S)-1-((1Z,3S,4Z,6S,7Z,9S,10Z,12S,13Z,15S,16Z)-1-((S)-1-((S)-2-((Z)-(((S)-1-(2-((Z)-((S)-2-((Z)-((S)-2-amino-1-hydroxy-4-(methylthio)butylidene)amino)-1-hydroxypropylidene)amino)acetyl)pyrrolidin-2-yl)(hydroxy)methylen | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@]2([H])CCCN2C(C/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CCSC)([H])C)=O)([H])CC3=CN=CN3)=O)([H])C(C)C)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/CC(N4CCC[C@@]4([H])/C(O)=N/[C@@](/C(O)=N | ||
| 分子式 | C75H118N20O22S | 分子量 | 1683.93 |
| 溶解度 | ≥ 179.9 mg/mL in DMSO with ultrasonic, <8.44 mg/mL in EtOH, ≥ 34.54 mg/mL in Water with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 593.8 μL | 2.9692 mL | 5.9385 mL |
| 5 mM | 118.8 μL | 593.8 μL | 1.1877 mL |
| 10 mM | 59.4 μL | 296.9 μL | 593.8 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet