pkcβ1

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.

Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α βI βII γ ε (IC50: 5 24 14 27 24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

HBDDE is a selective model inhibitor of the isoenzymes PKCα and PKCγ with IC 50 s of 43 μM and 50 μM, respectively.HBDDE has a higher affinity for PKCα PKCγ than the PKCδ, PKCβI, and PKCβII isoenzymes.HBDDE is a derivative of ellagic acid, which induces apoptosis in neuronal cells. HBDDE is a derivative of ellagic acid and induces apoptosis in neuronal cells.

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC) with IC50 values of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

Sotrastaurin (AEB071) is a potent pan-PKC inhibitor with Kis of 0.95 nM for PKCα, 0.64 nM for PKCβI, 2.1 nM for PKCδ, 3.2 nM for PKCε, 1.8 nM for PKCη, and 0.22 nM for PKCθ.

Evo312 is an inhibitor of protein kinase C beta I (PKCβI) with an IC50 of 117.34 nM and exhibits dose-dependent characteristics. It acts by inhibiting the expression of the PKCβI protein, which leads to cell cycle arrest and apoptosis in PANC-GR (gemcitabine-resistant pancreatic cancer cells). Evo312 also demonstrates antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR, with IC50 values of 0.08 μM and 0.07 μM respectively, while presenting an IC50 of 2.95 μM in normal human pancreatic ductal epithelial cells HPDE6-c7. Additionally, Evo312 has shown antitumor activity in a mouse xenograft model using PANC-GR cells.

Go6976 is a small molecule inhibitor of protein kinase C (PKC). Go6976 has been widely used in biomedical research as a tool to study the role of PKC in various physiological and pathophysiological processes.

PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).