PKC Inhibitor

Lyso-monosialoganglioside GM2 (LysoGM2) ammonium is a lysosphingolipid and protein kinase C inhibitor (IC₅₀: 50 μM). Lyso-monosialoganglioside GM2 ammonium can inhibit the binding of protein kinase C to Phorbol 12,13-dibutyrate (HY-18985). Lyso-monosialoganglioside GM2 ammonium is a specific biomarker for GM2 gangliosidosis. Lyso-monosialoganglioside GM2 ammonium can be used in the research of sphingolipidoses.

Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity.

Protein Kinase C (19-35) Peptide is the PKC pseudosubstrate inhibitor/region. Protein Kinase C (19-35) Peptide possibly blocks the substrate-binding site in its kinase domain, makes the cytoplasmic form of PKC inactive.

Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].

TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a K_i of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats.

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.

Aurothiomalate disodium acts as an inhibitor of PKCI and TrxR1. Aurothiomalate disodium disrupts the PKCI-Par6-Rac1 signaling pathway, and also inhibits TrxR1 activity, TNFα-induced NF-κB activation, and the expression of pro-inflammatory genes. Aurothiomalate disodium blocks Kras-mediated BASC expansion and lung tumor growth, inhibits anchorage-independent growth and tumorigenicity of lung cancer cells, and suppresses neutrophil chemotaxis, phagocytosis, and leukocyte extravasation. Aurothiomalate disodium can be used in research related to rheumatoid arthritis and non-small cell lung cancer.

aPKC-IN-1 (compound 1) is an atypical protein kinase C (aPKCζ) inhibitor. aPKC-IN-1 can be used for the study of a host of diseases involving increased vascular permeability and inflammation.

AS2521780 is a novel PKCθ selective inhibitor with an IC₅₀ of 0.48 nM.

ICP-103 (Compound 3K) is a highly selective protein kinase C (PKC) inhibitor with an IC₅₀ of 30 nM. ICP-103 is promising for research of cancers.

PKCε inhibitor peptide,myristoylated (Myr-PKCε-) is a cell permeable myristic acid conjugated PKC peptide inhibitor that attenuates NO release in cultured human umbilical vein endothelial cells (HUVECs).

Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC₅₀s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity.

(E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC₅₀ of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC₅₀ values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.

HA-100 hydrochloride is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.

Prkd1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prkd1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Aprinocarsen sodium scrambled negative control is the sequence scrambled negative control of Aprinocarsen sodium.

PICK1 PDZ-IN-1 (Compound 6b) is a selective and brain-penetrant protein interacting with C kinase 1 (PICK1) PDZ domain inhibitor with a K_i of 27.73 μM. PICK1 PDZ-IN-1 can competitively inhibit the interaction between PICK1 and the GluA2 subunit of AMPA receptors. PICK1 PDZ-IN-1 can increase the survival rate of HT22 cells and primary cortical neuron cells induced by glutamate and inhibit ROS production. PICK1 PDZ-IN-1 exhibits neuroprotective effect and reduces the area of cerebral infarction. PICK1 PDZ-IN-1 can be used for the research of ischemic stroke.

pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively blocks PICK1 interactions, caused the opposite effects on synaptic AMPAR function to PICK1 expression.

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.

PKC ζ pseudosubstrate, a PKC ζ inhibitor peptide, can be attached to cell permeabilization vector peptide.