GF109203X , PKC kinase inhibitor
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Catalog numberSIH-447-10MG
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PricePlease ask
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Size10 mg
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Stock availabilitIn StockIn Stock
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CAS number133052-90-1
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DescriptionPKC kinase inhibitor
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Molecular weight412,5 g/mol
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Primary research fieldsCell Signaling, Cancer, Apoptosis, Cancer Growth Inhibitors, Tyrosine Kinase Inhibitors
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Other name2-[1-(3-Dimethylaminopropyl)indol-3-yl]-3-(indol-3-yl) maleimide, 3-(N-[Dimethylamino]propyl-3-indolyl)-4-(3-indolyl)maleimide, 3-[1-[3-(Dimethylamino)propyl]1H-indol-3-yl]-4-(1Hindol-3-yl)1H-pyrrole-2,5dione, Bisindolylmaleimide I
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Product categorySmall Molecules
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Product typeInhibitor
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Chemical formulaC25H24N4O2
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OriginSynthetic
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Purity pourcentage≥98% (TLC)
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Soluble inSoluble in dimethyl formamide or DMSO (10 mg/ml, warm to 40°C and vortex well)
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Physical appearanceRed solid
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Storage recommendations-20ºC
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Shipping recommendationsShipped Ambient
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Safety informationClassification: Acute toxicity, Oral (Category 4), H302 Carcinogenicity (Category 2), H351 Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. Hazard statements: H302 Harmful if swallowed. H351 Suspected of causing cancer. Precautionary statements: P201 Obtain special instructions before use. P202 Do not handle until all safety precautions have been read and understood. P264 Wash skin thoroughly after handling. P270 Do not eat, drink or smoke when using this product. P281 Use personal protective equipment as required. P301 + P312 IF SWALLOWED: C all a POISON CENTER or doctor/ physician if you feel unwell. P308 + P313 IF exposed or concerned: Get medical advice/ attention. P330 Rinse mouth. P405 Store locked up. P501 Dispose of contents/ container to an approved waste disposal plant.
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PubChem number2396
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Scientific contextGF109203X is a very potent inhibitor of protein kinase C; it is selective for the α and β1 isoforms; this could lead to an increase in autophagy. GF109203X is also an inhibitor of glycogen synthase kinase-3 (GSK-3) and has anti-inflammatory effects. It has also been seen to inhibit telomerase activity and necrosis.
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Bibliography1. Toullec D., et al. (1991) J. Biol. Chem. 266(24): 15771–15781. 2. Jacobson P.B., et al. (1995) J. Pharma. Exp. Ther. 275(2): 995–1002. 3. Jiang Q., et al. (2011) Mol. Biol. Cell. 22(8): 1167–1180. 4. Kuchera S., et al. (1993) Agents and Actions. 39 Spec No: C169–173.
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Release date1-Oct-2014
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PubMed numberRefer to PubMed
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Tested applicationsTo be tested
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Tested reactivityTo be tested
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Representative figure legendChemical structure of GF109203X (SIH-447), a PKC kinase inhibitor. CAS #: 133052-90-1. Molecular Formula: C25H24N4O2. Molecular Weight: 412.5 g/mol. Chemical structure of GF109203X , a PKC kinase inhibitor (SIH-447). CAS # 133052-90-1. Molecular Formula: C25H24N4O2.
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Warning informationNon-hazardous
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Country of productionCanada
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Total weight kg0.25
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Net weight g0.01
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Additional descriptionTissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
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Gene target
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Gene symbolPRKCH, PRKD1, PRRT2, PRKDC
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Short nameGF109203X , PKC kinase inhibitor
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Alternative nameGF109203X , PKC phosphorylation catalyst suppressor
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Gene info
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Identity
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Gene
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Long gene nameprotein kinase C eta
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Synonyms gene
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Synonyms gene name
- protein kinase C, eta
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Synonyms
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GenBank acession
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Locus
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Discovery year1992-06-26
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- C2 domain containing protein kinases
- AGC family kinases
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VEGA ID
Gene info
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Identity
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Gene
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Long gene nameprotein kinase D1
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Synonyms gene
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Synonyms gene name
- protein kinase C, mu
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Synonyms
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Locus
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Discovery year1994-05-16
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Pleckstrin homology domain containing
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VEGA ID
Gene info
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Identity
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Gene
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Long gene nameproline rich transmembrane protein 2
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Synonyms gene
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Synonyms gene name
- infantile convulsions and paroxysmal choreoathetosis
- dystonia 10
- proline-rich transmembrane protein 2
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Synonyms
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Synonyms name
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GenBank acession
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Locus
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Discovery year2005-11-25
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- interferon induced transmembrane protein domain containing
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VEGA ID
Gene info
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Identity
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Gene
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Long gene nameprotein kinase, DNA-activated, catalytic subunit
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Synonyms gene
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Synonyms gene name
- protein kinase, DNA-activated, catalytic polypeptide
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Synonyms
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Synonyms name
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Locus
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Discovery year1993-11-09
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Entrez gene record
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Pubmed identfication
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RefSeq identity
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Classification
- Armadillo like helical domain containing
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VEGA ID
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Locus Specific Databases
