PKCβ inhibitor 1

PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> TGF-beta/Smad >> PKC

human PKCβ1:21 nM (IC50)

human PKCβ2:5 nM (IC50)

PKCα:331 nM (IC50)

PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner[2]. PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells[2]. PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells[2]. PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells[2]. PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation[2]. Cell Proliferation Assay[2] Cell Line: 2F7, BCBL-1 cells Concentration: 0, 5, 10, 20, and 30 μM Incubation Time: 48 hours Result: A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration. Apoptosis Analysis[2] Cell Line: 2F7 cells Concentration: 14 μM Incubation Time: 2-48 hours Result: Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment. Cell Cycle Analysis[2] Cell Line: BCBL-1 Cells Concentration: 15 μM (the IC50) Incubation Time: 2-48 hours Result: Inhibits cell cycle progression in 2F7 and BCBL-1 cells. Western Blot Analysis[2] Cell Line: BCBL-1 and 2F7 cell lines Concentration: 15 or 14 μM (at the IC50 respectively) Incubation Time: 2-48 hours Result: The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced.

[1]. Tanaka M, et al. Synthesis of anilino-monoindolylmaleimides as potent and selective PKCbeta inhibitors. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5171-4.

[2]. Saba NS, et al. Protein kinase C-beta inhibition induces apoptosis and inhibits cell cycle progression in acquired immunodeficiency syndrome-related non-hodgkin lymphoma cells. J Investig Med. 2012 Jan;60(1):29-38.