Drug intelligence / Profile preview

Gö6976

Development stage
Unknown
Lead developer
Gödecke
Modality
Small Molecules
Administration
Intraperitoneal, Oral, In Vitro
01

Overview

Gö6976 is a potent, cell-permeable, and selective small molecule inhibitor of conventional protein kinase C (cPKC) isoforms, including PKCα, PKCβ, and PKCγ, with IC50 values in the low nanomolar range. It belongs to the indolocarbazole chemical class and acts by competing with ATP for the kinase domain binding site. Unlike non-selective inhibitors like staurosporine, Gö6976 does not inhibit novel (nPKC) or atypical (aPKC) isoforms at concentrations that effectively block cPKCs. Additionally, it is a highly potent inhibitor of Protein Kinase D (PKD) and has demonstrated inhibitory activity against Janus kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Primarily utilized as a biochemical research tool, Gö6976 is used to investigate PKC-mediated pathways in cell differentiation, apoptosis, and oncogenesis, particularly in studies involving endometrial cancer and various leukemias.

Brand names
GO6976GO-6976GO 6976
Other names
12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazoleGoe 6976Goe6976Goe-6976
02

Targets

PRKCG (Protein kinase C gamma)JAK2 (Janus kinase 2)ENPP1NTRK1 (Tropomyosin-related receptor kinase A)JAK3 (Janus kinase 3)PRKCA (Protein kinase C alpha)NTRK2 (Tropomyosin-related kinase receptor type B)PRKCB (Protein kinase C beta)

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