PKCζ Inhibitor

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.

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

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.

CRT0066854 is a potent and selective atypical PKC isoenzymes 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.

PKCζ-IN-1 is a PKCζ-selective inhibitor with an IC₅₀ of 5.18 nM against human PKCζ. PKCζ-IN-1 also inhibits CDK2 with an IC₅₀ of 1.04 μM. PKCζ-IN-1 is applicable to research related to immune and inflammatory diseases.

PKCζ-IN-2 is an orally active, selective PKCζ inhibitor with an IC₅₀ of 0.1 nM. As an anti-inflammatory agent, PKCζ-IN-2 reduces joint swelling and ameliorates disease progression in a mouse collagen-induced arthritis model. PKCζ-IN-2 can be used for the research of rheumatoid arthritis.

ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC₅₀ of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.

PS432 is a PKC inhibitor with IC₅₀s of 16.9 μM (PKC_ι) and 18.5 μM (PKC_ζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models.

CRT0066854 hydrochloride is a potent and 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.

ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC₅₀ of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.

Niazirin is an orally active antioxidant. Niazirin can be isolated from Moringa oleifera Lam. Niazirin reduces the production levels of ROS and MDA, while increasing the levels of superoxide dismutase SOD and glutathione peroxidase GPx. Niazirin also abolishes high glucose-induced PKCζ activation and inhibits Nox4 protein expression. Niazirin exhibits excellent free radical scavenging activity. Niazirin significantly inhibits high glucose-induced proliferation of vascular smooth muscle cells. Niazirin can be used in the research of diabetic atherosclerosis.

PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKC_ζ (IC₅₀=10 μM) and PKC_η (IC₅₀=30 μM). PS315 has anti-cancer activity.