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Submit ReviewPKC 412
Description: Protein kinase C inhibitor
Alternative Names: CGP 41251
Chemical Name: [9S-(9α,10β,11β,13α)]-N-(2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methylbenzamide
Purity: ≥98% (HPLC)
Biological Activity for PKC 412
PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1, EGFR and MARK (microtubule affinity regulating kinase). Displays potent antitumor activity. Identified as targeting human host cell proteins that interact with SARS-CoV-2.
Technical Data for PKC 412
| M. Wt | 570.64 |
| Formula | C35H30N4O4 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 120685-11-2 |
| PubChem ID | 9829523 |
| InChI Key | BMGQWWVMWDBQGC-IIFHNQTCSA-N |
| Smiles | O=C(NC6)C1=C6C4=C3C2=C1C8=C(C=CC=C8)N2[C@](C[C@@H](N(C(C9=CC=CC=C9)=O)C)[C@H]7OC)([H])O[C@]7(C)N3C5=CC=CC=C45 |
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 PKC 412
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.56 | 15 |
Preparing Stock Solutions for PKC 412
The following data is based on the product molecular weight 570.64. 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 |
|---|---|---|---|
| 0.15 mM | 11.68 mL | 58.41 mL | 116.83 mL |
| 0.75 mM | 2.34 mL | 11.68 mL | 23.37 mL |
| 1.5 mM | 1.17 mL | 5.84 mL | 11.68 mL |
| 7.5 mM | 0.23 mL | 1.17 mL | 2.34 mL |
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Product Datasheets for PKC 412
References for PKC 412
References are publications that support the biological activity of the product.
Fabbro et al (2000) PKC412 - a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 15 17 PMID: 10888033
Tenzer et al (2001) The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C. Cancer Res. 61 8203 PMID: 11719451
Nakazono-Kusaba et al (2004) PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts. Eur.J.Pharmacol. 497 155 PMID: 15306200
Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859
If you know of a relevant reference for PKC 412, please let us know.
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5 Citations for PKC 412
Citations are publications that use Tocris products. Selected citations for PKC 412 include:
Kuan et al (2014) Ets and GATA Transcription Factors Play a Critical Role in PMA-Mediated Repression of the ckβ Promoter via the Protein Kinase C Signaling Pathway. PLoS One 9 e113485 PMID: 25490397
Moloney et al (2017) Subcellular localization of the FLT3-ITD oncogene plays a significant role in the production of NOX- and p22(phox)-derived reactive oxygen species in acute myeloid leukemia. Leuk Res 52 34 PMID: 27870947
Park et al (2016) Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS. Nat Immunol 17 914 PMID: 27270401
Woolley et al (2012) H2O2 production downstream of FLT3 is mediated by p22phox in the endoplasmic reticulum and is required for STAT5 signalling. PLoS One 7 e34050 PMID: 22807997
Wasag et al (2011) The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11). Haematologica 96 922 PMID: 21330321
Do you know of a great paper that uses PKC 412 from Tocris? Please let us know.
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