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 ActivityPKC 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.
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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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