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
Biological ActivityBroad 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.
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.
PKC412 - a protein kinase inhibitor with a broad therapeutic potential.
Fabbro et al.
Anticancer Drug Des., 2000;15:17
The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C.
Tenzer et al.
Cancer Res., 2001;61:8203
PKC412 induces apoptosis through a caspase-dependent mechanism in human keloid-derived fibroblasts.
Nakazono-Kusaba et al.
A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing.
Gordon et al.
Citations for PKC 412
The citations listed below are publications that use Tocris products. Selected citations for PKC 412 include:
5 Citations: Showing 1 - 5
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.
Authors: Moloney Et al.
Leuk Res 2017;52:34
Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS.
Authors: Park Et al.
Nat Immunol 2016;17:914
Ets and GATA Transcription Factors Play a Critical Role in PMA-Mediated Repression of the ckβ Promoter via the Protein Kinase C Signaling Pathway.
Authors: Kuan Et al.
PLoS One 2014;9:e113485
H2O2 production downstream of FLT3 is mediated by p22phox in the endoplasmic reticulum and is required for STAT5 signalling.
Authors: Woolley Et al.
PLoS One 2012;7:e34050
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).
Authors: Wasag Et al.
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