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 (3)
Literature

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 and EGFR. Displays potent antitumor activity.

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.

All Tocris products are intended for laboratory research use only.

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 solvent 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
1 mM 1.75 mL 8.76 mL 17.52 mL
5 mM 0.35 mL 1.75 mL 3.5 mL
10 mM 0.18 mL 0.88 mL 1.75 mL
50 mM 0.04 mL 0.18 mL 0.35 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for PKC 412, please let us know.

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Keywords: PKC 412, supplier, Broad, spectrum, protein, kinases, inhibitors, inhibits, conventional, PKC, PKC412, CGP41251, CGP, 41251, Protein, Kinase, C, Tocris Bioscience

3 Citations for PKC 412

Citations are publications that use Tocris products. Selected citations for PKC 412 include:

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

Kuan et al (2014) Ets and GATA Transcription Factors Play a Critical Role in PMA-Mediated Repression of the ck╬▓ Promoter via the Protein Kinase C Signaling Pathway. PLoS One 9 e113485 PMID: 25490397

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


Do you know of a great paper that uses PKC 412 from Tocris? If so please let us know.

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