pkcθ

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.

PKC-IN-1 is an ATP-competitive and reversible conventional PKC enzymes inhibitor (PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε with IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM, respectively).

VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ).

TCS 21311 (NIBR3049) is an effective and highly selective inhibitor of JAK3 (IC50: 8 nM). TCS 21311 inhibits PKCα, PKCθ, and GSK3β (IC50s: 13, 68, and 3 nM, respectively). It displays >100-fold selectivity over JAK1, JAK2, and TYK2.

PKC-theta inhibitor is PKC-θinhibitor, with an IC50 of 12 nM.

PKC-theta inhibitor hcl is a selective PKC-θinhibitor(IC50:12 nM).

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.

Myristoylated PKCθ pseudosubstrate peptide inhibitor is a synthetic peptide utilized to investigate the mechanism of action of protein kinase C theta (PKCθ) [1].

Myristoylated TFA, a PKCθ pseudosubstrate peptide inhibitor, is a synthetic peptide utilized for the study of PKCθ mechanisms of action.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.

20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway.

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator that inhibits α1-adrenoceptor-mediated positive inotropic effects in a concentration-dependent manner, induced by contraction of isolated rabbit vascular smooth muscle.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Go 6983 is a PKC inhibitor with IC50 values of 7, 7, 6, 10, and 60 nM for PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, respectively. Go 6983 has antitumor activity, cardiovascular protection, and protein kinase C inhibition.

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

PKC β pseudosubstrate acetate (PKC β pseudosubstrate acetate (172308-76-8 Free base)) is a selective cell-permeable inhibitor of PKC.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

CRT0066854 hydrochloride is an effective selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.

Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, demonstrating high specificity for divalent cations (Ca>Mg>Sr=Ba).

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen/glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε)/nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

HA-1004 is a inhibitor of PKG, PKA, PKC and MLC.

Bisindolylmaleimide VIII (Ro-31-7549) is a selective and potent protein kinase C (PKC) inhibitor with good inhibition of PKC-α, PKC-β I, PKC-β II, PKC-γ, and PKC-ε.Bisindolylmaleimide VIII Bisindolylmaleimide VIII inhibits T cell-mediated autoimmune diseases and enhances Fas-mediated apoptosis through a protein kinase C-independent mechanism.

TV 3279 is a novel ChE-MAI inhibitor , and the neuroprotective properties depend on their ability to induce the anti-apoptotic proteins PKC, Bcl-2, Bcl-x, and SOD, and to block the nuclear translocation of the pro-apoptotic enzyme glyceraldehyde phosphate dehydrogenase in PC-12 and neuroblastoma cells.