PKCβ Inhibitor

PKCβ Inhibitors (27):

Cat. No.	Product Name	Effect	Purity

HY-13689

Go 6983	Inhibitor	99.32%
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC₅₀ of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.

HY-10230

Midostaurin	Inhibitor	99.91%
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, VEGFR2/KDR/Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/Flt-1/2 with IC₅₀s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.

HY-13867

Bisindolylmaleimide I	Inhibitor	98.66%
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.

HY-18980

Rottlerin	Inhibitor	98.09%
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC₅₀ values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.

HY-10343

Sotrastaurin	Inhibitor	99.71%
Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is 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-169006

Evo312	Inhibitor
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC₅₀ is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC₅₀ of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC₅₀ of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model.

HY-129624

Bisindolylmaleimide VIII	Inhibitor
Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC₅₀ of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC₅₀s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.

HY-15727

Afuresertib	Inhibitor	99.53%
Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.

HY-10342

Enzastaurin	Inhibitor	99.92%
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

HY-13866

Ro 31-8220 mesylate	Inhibitor	99.57%
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

HY-10195

Ruboxistaurin	Inhibitor	99.90%
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (K_i=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC₅₀ of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC₅₀ of 5.9 nM.

HY-13335

PKCβ inhibitor 1	Inhibitor	99.40%
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).

HY-16903

PKC-IN-1	Inhibitor	98.79%
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with K_is 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 K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.

HY-10195B

Ruboxistaurin hydrochloride	Inhibitor	99.94%
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (K_i=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC₅₀ of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC₅₀ of 5.9 nM.

HY-129624A

Bisindolylmaleimide VIII acetate	Inhibitor	99.68%
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC₅₀ of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC₅₀s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.

HY-13867A

Bisindolylmaleimide I hydrochloride	Inhibitor	99.18%
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.

HY-122246

ML192	Inhibitor
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.

HY-10195A

Ruboxistaurin mesylate	Inhibitor	99.87%
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC₅₀ values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes.

HY-117610A

Bisindolylmaleimide XI hydrochloride	Inhibitor	≥98.0%
Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC₅₀s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.

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