PKC 412

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Cat.No. 2992 - PKC 412 | C35H30N4O4 | CAS No. 120685-11-2
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)
Datasheet
Citations (5)
Reviews
Literature (3)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 8.56 15

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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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