R18 TFA是一种14-3-3的肽类拮抗剂，KD值为70-90nM。
Sample solution is provided at 25 µL, 10mM.
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R18 TFA is a peptide antagonist of 14-3-3, with KD of 70-90nM [1]. R18 TFA can inhibit all members of the 14-3-3 protein family with a very similar affinity coefficient, and effectively utilize the amphiphilicity of the 14-3-3 binding channel to competitively inhibit phosphorylation and non-14-3-3-dependent protein-protein interactions [2]. Disruption of 14-3-3 via the R18 TFA switches nerve growth factor- and myelin-associated glycoprotein-dependent repulsion to attraction in rat DRG neurons [3]. The R18 TFA has been widely used to disrupt the binding of 14-3-3 to the ligands, thereby screening out the proteins that are regulated by 14-3-3[4].
In vitro, R18 TFA treatment at 8μM for 48 hours significantly inhibited the viability of MMQ cells and reduced the expression of 14-3-3η[5].
References:
[1] Wang B, Yang H, Liu Y C, et al. Isolation of high-affinity peptide antagonists of 14-3-3 proteins by phage display[J]. Biochemistry, 1999, 38(38): 12499-12504.
[2] Liu J, Cao S, Ding G, et al. The role of 14‐3‐3 proteins in cell signalling pathways and virus infection[J]. Journal of cellular and molecular medicine, 2021, 25(9): 4173-4182.
[3] Kent C B, Shimada T, Ferraro G B, et al. 14-3-3 proteins regulate protein kinase a activity to modulate growth cone turning responses[J]. Journal of Neuroscience, 2010, 30(42): 14059-14067.
[4] Repton C, Cullen C F, Costa M F A, et al. The phospho-docking protein 14-3-3 regulates microtubule-associated proteins in oocytes including the chromosomal passenger Borealin[J]. PLoS Genetics, 2022, 18(6): e1009995.
[5] Zhao S, Li B, Li C, et al. The apoptosis regulator 14-3-3η and its potential as a therapeutic target in pituitary oncocytoma[J]. Frontiers in endocrinology, 2019, 10: 797.
R18 TFA是一种14-3-3的肽类拮抗剂，KD值为70-90nM[1]。R18 TFA能以非常相似的亲和系数抑制14-3-3蛋白家族的所有成员，并有效利用14-3-3结合通道的两亲性，竞争性地抑制磷酸化及非14-3-3依赖的蛋白质-蛋白质相互作用[2]。通过R18 TFA破坏14-3-3，可使大鼠背根神经节神经元中神经生长因子和髓鞘相关糖蛋白依赖性排斥转变为吸引[3]。R18 TFA已被广泛用于破坏14-3-3与配体的结合，从而筛选出受14-3-3调控的蛋白质[4]。
在体外，使用8µM的R18 TFA处理48小时，显著抑制了MMQ细胞的活力，并降低了14-3-3η的表达[5]。
| Cell experiment [1]: | |
Cell lines | MMQ cells |
Preparation Method | MMQ cells were maintained in F12K medium supplemented with 2.5% fetal bovine serum (FBS) and 15% horse medium in humidified atmosphere with 5% CO2 at 37°C. Cells were seeded in 96-well plates at a density of 1×104 cells per well. After 24h, cells were incubated in the presence of 8μM R18 TFA, or the vehicle alone (DMSO) for 48h. Cell proliferation was measured. |
Reaction Conditions | 8μM; 48h |
Applications | R18 TFA treatment inhibited the cell viability of MMQ cells. |
References: | |
| Cas No. | SDF | ||
| 别名 | PHCVPRDLSWLDLEANMCLP TFA | ||
| 分子式 | C103H158F3N27O31S3 | 分子量 | 2423.73 |
| 溶解度 | Water : < 0.1 mg/mL (ultrasonic) (insoluble) | 储存条件 | -80°C, away from moisture |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 412.6 μL | 2.0629 mL | 4.1259 mL |
| 5 mM | 82.5 μL | 412.6 μL | 825.2 μL |
| 10 mM | 41.3 μL | 206.3 μL | 412.6 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。
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