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Submit ReviewJNJ 10198409
Description: Potent PDGFRα and PDGFRβ inhibitor; also inhibits c-Abl, Lck, c-Src and Fyn kinases
Chemical Name: N-(3-Fluorophenyl)-1,4-dihydro-6,7-dimethoxyindeno[1,2-c]pyrazol-3-amine
Purity: ≥98% (HPLC)
Biological Activity for JNJ 10198409
JNJ 10198409 is a potent platelet-derived growth factor receptor (PDGFR) inhibitor (IC50 values are 4.2 and 45 nM for PDGFRβ and PDGFRα, respectively). Also inhibits c-Abl, Lck, c-Src and Fyn kinases (IC50 values are 22, 100, 185 and 378 nM respectively). Displays antiproliferative activity in multiple tumor cell lines. Accelerates down regulation of fibroblast genes in transdifferentiation of human fibroblasts into functional cardiomyocytes, within 9C cocktail.
For more information about how JNJ 10198409 may be used, see our protocol: Converting Fibroblasts into Cardiomyocytes (9C Cocktail)
Licensing Information
Sold with the permission of Janssen Pharmaceutica N.V.
Compound Libraries for JNJ 10198409
JNJ 10198409 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 10198409
| M. Wt | 325.34 |
| Formula | C18H16FN3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 627518-40-5 |
| PubChem ID | 9797370 |
| InChI Key | ZDNURMVOKAERHZ-UHFFFAOYSA-N |
| Smiles | COC1=C(OC)C=C2C(CC3=C2NN=C3NC2=CC(F)=CC=C2)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 10198409
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.51 | 20 | |
| ethanol | 32.53 | 100 |
Preparing Stock Solutions for JNJ 10198409
The following data is based on the product molecular weight 325.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.07 mL | 15.37 mL | 30.74 mL |
| 5 mM | 0.61 mL | 3.07 mL | 6.15 mL |
| 10 mM | 0.31 mL | 1.54 mL | 3.07 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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Product Datasheets for JNJ 10198409
References for JNJ 10198409
References are publications that support the biological activity of the product.
Ho et al (2005) (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J.Med.Chem. 29 8163 PMID: 16366598
Cao et al (2016) Conversion of human fibroblasts into functional cardiomyocytes by small molecules. Science. 352 1216 PMID: 27127239
If you know of a relevant reference for JNJ 10198409, please let us know.
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Keywords: JNJ 10198409, JNJ 10198409 supplier, JNJ10198409, stem, cell, reprogramming, 9C, cocktail, cardiomyocytes, myocytes, platelet-derived, growth, factor, receptor, alpha, beta, inhibitors, inhibits, PDGFR, PDGFRb, PDGFRa, transdifferentiation, Src, Kinases, Other, Stem, Cell, Reprogramming, Cardiomyocyte, Cells, 6976, Tocris Bioscience
8 Citations for JNJ 10198409
Citations are publications that use Tocris products. Selected citations for JNJ 10198409 include:
Zhihui et al (2011) Mechanical regulation of glycogen synthase kinase 3β (GSK3β) in mesenchymal stem cells is dependent on Akt protein serine 473 phosphorylation via mTORC2 protein. J Biol Chem 286 39450-6 PMID: 21956113
Stewart O et al (2015) Conventional protein kinase C isoforms differentially regulate ADP- and thrombin-evoked Ca2+ signalling in human platelets. Cell Calcium 58 577-88 PMID: 26434503
Q Jane et al (2013) Protein kinase D promotes airway epithelial barrier dysfunction and permeability through down-regulation of claudin-1. J Biol Chem 288 37343-54 PMID: 24265314
Ulrich et al (2019) Self-organization of modular network architecture by activity-dependent neuronal migration and outgrowth. Elife 8 PMID: 31526478
Stephen H et al (2016) Tyrosine Binding Protein Sites Regulate the Intracellular Trafficking and Processing of Amyloid Precursor Protein through a Novel Lysosome-Directed Pathway. PLoS One 11 e0161445 PMID: 27776132
Anisur et al (2014) Mesenchymal chemotaxis requires selective inactivation of myosin II at the leading edge via a noncanonical PLCγ/PKCα pathway. Dev Cell 31 747-60 PMID: 25482883
Donghong et al (2020) Anaplastic Lymphoma Kinase Regulates Internalization of the Dopamine D2 Receptor. Mol Pharmacol 97 123-131 PMID: 31734646
F et al (2000) Protein kinase C activity modulates dendritic differentiation of rat Purkinje cells in cerebellar slice cultures. Eur J Neurosci 12 1993-2005 PMID: 10886339
Do you know of a great paper that uses JNJ 10198409 from Tocris? Please let us know.
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Protocols for JNJ 10198409
The following protocol features additional information for the use of JNJ 10198409 (Cat. No. 6976).
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