PPIase-Parvulin Inhibitor (Synonyms: HIC 016C,PiB) |
| Catalog No.GC12953 |
PPIases Pin1 and Pin4 inhibitor,cell-permeable
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 64005-90-9
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | HIC 016C,PiB | ||
| 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 | ||
| Formula | C22H18N2O8 | M.Wt | 438.4 |
| Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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