FJ9
Based on 1 Customer Validation
FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma.
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- Pureté: 98.86%
- CAS No.: 873841-43-1
- Formule: C23H27NO3
- Masse moléculaire:365.47
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
FJ9 (Compound 1) inhibits the interaction between GST-fused human NHERF1 PDZ1 domain and biotinylated β2AR carboxy-terminal peptide with an IC50 of 1540 μM[1].
FJ9 inhibits the interaction between GST-fused human NHERF1 PDZ2 domain and biotinylated CFTR carboxy-terminal peptide with an IC50 of 160 μM[1].
FJ9 (0.1-1000 μM) competitively inhibits Frz7 peptide binding to purified human DVL1 PDZ domain with a Ki of 63 μM and to purified human DVL3 PDZ domain with a Ki of 29 μM[2].
FJ9 (100-300 μM; 24 hours) penetrates HEK293T cells and disrupts the intracellular interaction between HA-tagged mouse DVL1 and myc-tagged human Frz7 at concentrations of 100 μM and 300 μM[2].
FJ9 (100-300 μM; 48 hours) dose-dependently down-regulates cytosolic β-catenin levels in hTERT-immortalized LP9 mesothelial cells stably expressing full-length mouse DVL1, but not in control LP9 cells or LP9 cells expressing PDZ domain-deleted mouse DVL1[2].
FJ9 (100-300 μM; 24 hours) dose-dependently inhibits constitutive Tcf transcriptional activity in HCT116 p53-/- colon cancer cells, reducing TOPflash reporter activity while minimally affecting FOPflash reporter activity[2].
FJ9 (30-100 μM; 1-2 days) down-regulates canonical Wnt signaling target proteins (cyclin D1, c-myc, survivin) and mRNA (cyclin D1, survivin) in HCT116 p53-/- colon cancer cells, and down-regulates survivin protein in NCI-H1703 non-small cell lung cancer cells[2].
FJ9 (30-100 μM; 24 hours) does not affect JNK activation in mDVL1-transfected HeLa cells after 24 hours of treatment at 30 μM and 100 μM[2].
FJ9 (86-100 μM; 3 to 6 days) induces significant apoptosis in LOX melanoma, NCI-H460 non-small cell lung cancer, and NCI-H1703 non-small cell lung cancer cells, but has no apoptotic effect on NCI-H28 mesothelioma cells or normal NHBE and SAEC cells, after 3 to 6 days of treatment at 86 to 100 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells transiently expressing HA-tagged mouse DVL1 and myc-tagged human Frz7
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Concentration:100 μM; 300 μM
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Incubation Time:24 h
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Result:Diminished the formation of the intracellular DVL1-Frz7 complex at concentrations above the in vitro Ki value, as shown by reduced detection of myc-tagged Frz7 in anti-HA immunoprecipitates.
Left whole lysate myc-hFrz7 levels consistent.
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Cell Line:hTERT-immortalized LP9 mesothelial cells stably expressing empty vector, full-length mouse DVL1, or PDZ domain-deleted mouse DVL1 (ΔPDZ-DVL1)
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Concentration:100 μM; 300 μM
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Incubation Time:48 hours
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Result:Causes a dose-dependent down-regulation of cytosolic β-catenin exclusively in LP9 cells stably expressing full-length DVL1.
Causes no significant change in cytosolic β-catenin levels in control empty vector-expressing cells or ΔPDZ-DVL1-expressing cells.
Causes no significant cell death or morphologic changes in any cell line.
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Cell Line:HCT116 p53-/- colon cancer cells; NCI-H1703 non-small cell lung cancer cells
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Concentration:30 μM; 100 μM
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Incubation Time:2 days
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Result:Down-regulated canonical Wnt signaling target proteins (cyclin D1, c-myc, survivin) in HCT116 p53-/- colon cancer cells, and down-regulated survivin protein in NCI-H1703 non-small cell lung cancer cells
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Cell Line:HCT116 p53-/- colon cancer cells; NCI-H1703 non-small cell lung cancer cells
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Concentration:30 μM; 100 μM
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Incubation Time:1 day
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Result:Down-regulated cyclin D1 and survivin in HCT116 p53-/- colon cancer cells.
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Cell Line:HeLa cells transiently transfected with mouse DVL1
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Concentration:30 μM; 100 μM
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Incubation Time:24 hours
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Result:Has no effect on the dual phosphorylation (activation) of JNK in mDVL1-transfected HeLa cells, indicating no impact on non-canonical Wnt signaling mediated by JNK.
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Cell Line:LOX melanoma cells, NCI-H460 non-small cell lung cancer cells, NCI-H1703 non-small cell lung cancer cells, NCI-H28 mesothelioma cells, normal human bronchial epithelial (NHBE) cells, normal human small airway epithelial (SAEC) cells
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Concentration:86 μM; 100 μM
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Incubation Time:3 days; 4 days
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Result:Induces significant apoptosis in LOX, H460, and H1703 tumor cells with intact β-catenin signaling.
Neither suppresses growth nor induces apoptosis in H28 mesothelioma cells with a homozygous β-catenin gene deletion.
Has minimal effect on normal NHBE and SAEC cells which do not express Wnt-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSWNU-M (6-week-old female, injected s.c. with 4 million H460 tumor cells)[2]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Significantly inhibited growth of H460 tumor xenografts.
Reduced mean tumor volume to ~300 mm3 on day 12 (vs ~400 mm3 for vehicle control).
Reduced mean tumor volume to ~275 mm3 on day 14 (vs ~475 mm3 for vehicle control).
Reduced mean tumor volume to ~325 mm3 on day 16 (vs ~700 mm3 for vehicle control).
Caused no significant mouse weight loss (<5%).
Chemical Information
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CAS No. 873841-43-1
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Appearance Solid
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Masse moléculaire 365.47
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Formule C23H27NO3
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Color White to off-white
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SMILES
O=C(C1=CC2=C(NC(C(CCCC)O)=C2CCC3=CC=CC=C3)C=C1C)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (273.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.84 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Mayasundari A, et al. Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains. Bioorg Med Chem Lett. 2008;18(3):942-945. [Content Brief]
[2]. Fujii N, et al. An antagonist of dishevelled protein-protein interaction suppresses beta-catenin-dependent tumor cell growth. Cancer Res. 2007;67(2):573-579. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7362 mL | 13.6810 mL | 27.3620 mL | 68.4051 mL |
| 5 mM | 0.5472 mL | 2.7362 mL | 5.4724 mL | 13.6810 mL | |
| 10 mM | 0.2736 mL | 1.3681 mL | 2.7362 mL | 6.8405 mL | |
| 15 mM | 0.1824 mL | 0.9121 mL | 1.8241 mL | 4.5603 mL | |
| 20 mM | 0.1368 mL | 0.6841 mL | 1.3681 mL | 3.4203 mL | |
| 25 mM | 0.1094 mL | 0.5472 mL | 1.0945 mL | 2.7362 mL | |
| 30 mM | 0.0912 mL | 0.4560 mL | 0.9121 mL | 2.2802 mL | |
| 40 mM | 0.0684 mL | 0.3420 mL | 0.6841 mL | 1.7101 mL | |
| 50 mM | 0.0547 mL | 0.2736 mL | 0.5472 mL | 1.3681 mL | |
| 60 mM | 0.0456 mL | 0.2280 mL | 0.4560 mL | 1.1401 mL | |
| 80 mM | 0.0342 mL | 0.1710 mL | 0.3420 mL | 0.8551 mL | |
| 100 mM | 0.0274 mL | 0.1368 mL | 0.2736 mL | 0.6841 mL |
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