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NFAT Inhibitor-1

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Chemical Structure| 249537-73-3 同义名 : VIVIT peptide;NFAT Inhibitor
CAS号 : 249537-73-3
货号 : A725430
分子式 : C75H120N20O22S
纯度 : 98%
分子量 : 1685.941
MDL号 : MFCD02683959
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:6个月
溶解度 :

H2O: 100 mg/mL(59.31 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 The nuclear factor of activated T cells (NFAT) is a family of transcription factors that regulate immune responses and adaptive response in skeletal and cardiac muscle. NFAT inhibitor (VIVIT peptide) is a cell-permeable peptide that selectively inhibits calcineurin-mediated dephosphorylation of NFAT[1]. In peripheral blood CD14+ monocytes isolated from rheumatoid arthritis patients, treatment with 10μM of NFAT inhibitor plus 100ng/mL of recombinant human RANKL and 50ng/mL of M‐CSF for 24h significantly inhibited nuclear translocation of NFATc1, but not that of peroxisome proliferator-activated receptor γ coactivator 1β. Long-term (21 days) treatment with NFAT inhibitor in combination with M‐CSF and RANKL significantly inhibited the cytoplasmic levels of cathepsin K, tartrate‐resistant acid phosphatase, and matrix metalloproteinase 9[2]. Intraperitoneal administration of NFAT (10mg/kg) once daily for 2 days prevented T-cell activation and proliferation in C3H/HeN mice[3].
作用机制 NFAT inhibitor potently and selectively inhibits the NFAT-calcineurin interaction without affecting calcineurin phosphatase activity. It was developed based on the conserved calcineurin docking site of NFAT[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.59mL

0.12mL

0.06mL

2.97mL

0.59mL

0.30mL

5.94mL

1.19mL

0.59mL
参考文献

[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. doi:10.1126/science.285.5436.2129

[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. doi:10.1002/art.40868

[3]Noguchi H, Matsushita M, Okitsu T, et al. A new cell-permeable peptide allows successful allogeneic islet transplantation in mice. Nat Med. 2004;10(3):305-309.