2. Signaling Pathways
  3. Epigenetics
    TGF-beta/Smad
  4. PKC
  5. PKCθ Isoform
  6. PKCθ Inhibitor

PKCθ Inhibitor

PKCθ Inhibitors (17):

Cat. No. Product Name Effect Purity
  • HY-10343
    Sotrastaurin
    		Inhibitor 99.71%
    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
  • HY-15727
    Afuresertib
    		Inhibitor 99.53%
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
  • HY-101569
    Darovasertib
    		Inhibitor 99.42%
    Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.
  • HY-132304
    CC-90005
    		Inhibitor 99.98%
    CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression.
  • HY-164756
    PKCTheta-IN-2
    		Inhibitor 99.49%
    PKCTheta-IN-2 (compound 14) is a potent and selective PKCθ inhibitor with an IC50 of 0.25 nM. PKCTheta-IN-2 shows good selectivity over a wide range of kinases, including the PKC subfamily (30 kinases). PKCTheta-IN-2 inhibits the IL-2 production in a mouse (IC50 of 682 nM).
  • HY-112782
    VTX-27
    		Inhibitor 99.02%
    VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
  • HY-112681
    PKC-theta inhibitor 2
    		Inhibitor 99.37%
    PKC-theta inhibitor 2 is a selective PKC-θinhibitor, with an IC50 of 12 nM.
  • HY-16903
    PKC-IN-1
    		Inhibitor 98.79%
    PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
  • HY-15727A
    Afuresertib hydrochloride
    		Inhibitor 99.95%
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
  • HY-108264
    TCS 21311
    		Inhibitor 99.18%
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
  • HY-126328
    PKC-theta inhibitor 1
    		Inhibitor 99.73%
    PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
  • HY-148561
    CDK8-IN-12
    		Inhibitor 99.74%
    CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent.
  • HY-162234
    PKCTheta-IN-1
    		Inhibitor
    PKCTheta-IN-1 (Compound 19) is a selective macrocyclic PKCTheta inhibitor with IC50 value of 0.1 nM.
  • HY-139467
    PF-04577806
    		Inhibitor
    PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.
  • HY-12663
    AS2521780
    		Inhibitor
    AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
  • HY-139466
    PF-03622905
    		Inhibitor
    PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases.
  • HY-149054
    GSK-3β inhibitor 13
    		Inhibitor
    GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease.