PPIase-Parvulin Inhibitor
(Synonyms: 1,3,6,8-四氢-1,3,6,8-四氧代-苯并[LMN][3,8]菲咯啉-2,7-二乙酸2,7-二乙酯,HIC 016C,PiB) 目录号 : GC12953
A cell-permeable Pin1 and Pin4 inhibitor
Cas No.:64005-90-9
Sample solution is provided at 25 µL, 10mM.
Targets: Pin1 and Pin4
IC50: 1.5 and 1.0 μM for Pin1 and Pin4, respectively.
PPIase-Parvulin Inhibitor is a cell-permeable inhibitor of the PPIases Pin1 and Pin4, with the IC50 values of 1.5 and 1.0 μM, respectively [1].
In Vitro: PPIase-Parvulin Inhibitor could significantly inhibit a number of cancer cell lines such as HSC2, HSC4, HCT116, SKOV3 that overexpressed Pin1 and Pin4, with the IC50 values ranging from 2-5 μM, while cancer cell lines with a low expression of Pin1 such as HLE and HepG2 were less sensitive to PPIase-Parvulin Inhibitor [1]. Besides, 0.5 μg/ml PPIase-Parvulin Inhibitor could reduce MCF10A-Myc cells colony formation which was induced by Pin1 overexpression [2]. Furthermore, in NOP6 mouse mammary tumor cells, 1.5 μM PPIase-Parvulin Inhibitor could significantly impair mammosphere formation efficiency (MFE) at the M2 level [3].
In Vivo: No data available recently.
Clinical trial: No data available recently.
References:
[1] Uchida T, Takamiya M, Takahashi M, et al. Pin1 and Par14 Peptidyl Prolyl Isomerase Inhibitors Block Cell Proliferation[J]. Chemistry & Biology, 2003, 10(1):15.
[2] Farrell A S, Pelz C, Wang X, et al. Pin1 Regulates the Dynamics of c-Myc DNA Binding To Facilitate Target Gene Regulation and Oncogenesis[J]. Molecular and Cellular Biology, 2013, 33(15): 2930-2949.
[3] Rustighi A, Zannini A, Tiberi L, et al. Prolyl‐isomerase Pin1 controls normal and cancer stem cells of the breast[J]. Embo Molecular Medicine, 2014, 6(1): 99-119.
Cas No. | 64005-90-9 | SDF | |
别名 | 1,3,6,8-四氢-1,3,6,8-四氧代-苯并[LMN][3,8]菲咯啉-2,7-二乙酸2,7-二乙酯,HIC 016C,PiB | ||
化学名 | 1,3,6,8-tetrahydro-1,3,6,8-tetraoxo-benzo[lmn][3,8]phenanthroline-2,7-diacetic acid, 2,7-diethyl ester | ||
Canonical SMILES | O=C1N(CC(OCC)=O)C(C2=CC=C(C3=C4C=CC1=C23)C(N(CC(OCC)=O)C4=O)=O)=O | ||
分子式 | C22H18N2O8 | 分子量 | 438.4 |
溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 2.281 mL | 11.4051 mL | 22.8102 mL |
5 mM | 0.4562 mL | 2.281 mL | 4.562 mL |
10 mM | 0.2281 mL | 1.1405 mL | 2.281 mL |
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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