| CAS NO: | 64005-90-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 438.4 |
| Cas No. | 64005-90-9 |
| Formula | C22H18N2O8 |
| Synonyms | HIC 016C,PiB |
| Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| Chemical Name | 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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