JP-153
Based on 1 Customer Validation
JP-153 is a FAK-paxillin interaction inhibitor. JP-153 prevents the binding of the paxillin LD motif to the FAK FAT domain and disrupts the Src/FAK/paxillin focal adhesion complex, thereby reducing paxillin phosphorylation, YAP nuclear accumulation, and Akt activation. JP-153 selectively impairs mechanotaxis. JP-153 inhibits stiff matrix/TGF-β-induced myofibroblast differentiation and tumor cell invasion, and reduces tumor fibrosis and lung metastasis. JP-153 reduces Bleomycin-induced fibrosis. JP-153 inhibits VEGF-induced retinal endothelial proliferation, migration, and invasion, as well as pathological retinal neovascularization in oxygen-induced retinopathy. JP-153 attenuates tumor fibrosis and lung metastasis in KPC689 subcutaneous tumors. JP-153 can be used for research on pulmonary fibrosis, metastatic pancreatic cancer, and pathological retinal neovascularization.
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- Pureté : 99.45%
- CAS No.: 1802937-26-3
- Formule: C21H19NO5
- Masse moléculaire:365.38
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
JP-153 (0.5-1 µM; 24 h) reduces the number of viable primary human retinal endothelial cells at 0.5 and 1 µM under VEGF stimulation[2].
JP-153 (1 µM; 1 h) reduces VEGF-induced paxillin Y118 phosphorylation in primary human retinal endothelial cells without affecting unstimulated constitutive levels[2].
JP-153 (1 µM; 1 h pretreatment) uncouples paxillin Y118 and Akt signaling from FAK phosphorylation in VEGF-stimulated primary human retinal endothelial cells[2].
JP-153 (0.1-10 µM; 24 h) inhibits VEGF-induced migration of primary human retinal endothelial cells in the scratch wound healing assay[2].
JP-153 (0.10-0.50 µM; 24 h) inhibits VEGF-induced Transwell invasion of primary human retinal endothelial cells[2].
JP-153 (10 nM-10 µM; migration 24 h; proliferation/viability 48 h) selectively inhibits durotaxis of human lung fibroblasts without affecting chemotaxis, haptotaxis, survival, or proliferation[1].
JP-153 (100 nM; 24 h; 300 nM-1 µM after exposure) prevents stiffness-dependent myofibroblast activation but does not reverse established myofibroblast differentiation in human lung fibroblasts[1].
JP-153 blocks FAK-paxillin-YAP mechanotransduction during durotactic migration of human lung fibroblasts[1].
JP-153 inhibits durotaxis migration of primary fibrotic lung fibroblasts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human lung fibroblasts
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Concentration:0, 0.01, 0.1, 0.3, 1 µM
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Incubation Time:24 h
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Result:Reduced phospho-paxillin Y31 without affecting Y397 FAK autophosphorylation.
Proximity ligation assay supported disruption of FAK-paxillin complexes.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N (male, 6-8 weeks old)[1]
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Dosage:5 mg/kg
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Administration:topical microemulsion to shaved neck skin; daily; prophylactic day 0-21 and post-onset day 10-21
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Result:Reduced bleomycin-induced lung fibrosis at day 21.
Inhibited the FAK-paxillin Y31/118 pathway in lung tissue.
Reduced α-SMA+ myofibroblasts per cluster and reduced ECM deposition and hydroxyproline levels.
Post-onset dosing from day 10 to day 21 also reduced established lung fibrosis.
Did not alter total or active TGF-β levels, alveolar-capillary barrier permeability at day 7, or leukocyte recruitment in BAL fluid.
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Animal Model:C57BL/6J[1]
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Dosage:5 mg/kg
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Administration:topical microemulsion; daily; 21 days
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Result:Did not affect overall primary tumour growth, angiogenesis, or basement membrane protein levels.
Reduced tumour fibrosis.
Increased CD8+ cytotoxic T cells in the primary tumour.
Reduced lung metastases compared with vehicle control.
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Animal Model:C57BL/6N (postnatal pups P7-P17)[2]
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Dosage:0.5 mg/kg; 5.0 mg/kg
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Administration:topical ocular application to both eyes; once daily; from P12 to P17
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Result:In OIR mice, retinal neovascularization was reduced by 40% at 0.5 mg/kg and by 45% at 5.0 mg/kg compared with vehicle-treated eyes.
Avascular area was increased only at 5.0 mg/kg compared with vehicle.
- Spheroid/Tumor Organoid Invasion Assay
- Western Blot
- Ex Vivo Tissue Slice/Explant Invasion Assay
- Collagen: Sirius Red Staining
- Patient-Derived Organoid Invasion Assay
- Cell migration
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- 3D Tumor Spheroid Invasion Assay
- Matrigel Transwell/Boyden Chamber Invasion Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- Invadopodia/Fluorescent Gelatin Degradation Assay
- Fibrosis/Collagen Morphometry
- How to Select the Route of Administration for Mammals
- Tail-Vein Experimental Metastasis Xenograft
- Organotypic 3D Invasion Assay
- Cell invasion
- Matrigel/ECM Transwell Invasion Assay
- Glioma/Brain Tumor 3D Invasion Assay
- Protocol for Kinase activity and phosphorylation assays
- Orthotopic Cell-Line Xenograft
- 3D Collagen/Hydrogel Matrix Invasion Assay
Chemical Information
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CAS No. 1802937-26-3
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Appearance Solid
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Masse moléculaire 365.38
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Formule C21H19NO5
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Color Pale purple to light pink
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SMILES
O=C1OC(C2=CC(OC)=C(OC)C(OC)=C2)C3=CC=C4C=CC=CC4=C3N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : ≥ 200 mg/mL (547.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 |
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| DMSO | 1 mM | 2.7369 mL | 13.6844 mL | 27.3688 mL | 68.4219 mL |
| 5 mM | 0.5474 mL | 2.7369 mL | 5.4738 mL | 13.6844 mL | |
| 10 mM | 0.2737 mL | 1.3684 mL | 2.7369 mL | 6.8422 mL | |
| 15 mM | 0.1825 mL | 0.9123 mL | 1.8246 mL | 4.5615 mL | |
| 20 mM | 0.1368 mL | 0.6842 mL | 1.3684 mL | 3.4211 mL | |
| 25 mM | 0.1095 mL | 0.5474 mL | 1.0948 mL | 2.7369 mL | |
| 30 mM | 0.0912 mL | 0.4561 mL | 0.9123 mL | 2.2807 mL | |
| 40 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7105 mL | |
| 50 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3684 mL | |
| 60 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1404 mL | |
| 80 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8553 mL | |
| 100 mM | 0.0274 mL | 0.1368 mL | 0.2737 mL | 0.6842 mL |
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