human pkcα

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).

NNK is a nitrosated derivative of nicotine that activates the ERK1/2 and PKCα signaling pathways, induces Bcl2 phosphorylation at Ser70, and activates c-Myc at Thr58 and Ser62, thereby promoting the proliferation and survival of human lung cancer cells, and is commonly used to establish lung cancer mouse models.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Balanol is an ATP-competitive Protein Kinase C and Protein Kinase A inhibitor.

CP21R7 (CP21) is an effective and specific GSK3β inhibitor. It is used as an activator of stem cells prior to the induction of differentiation of stem cells to smooth muscle and endothelial cells. CP21R7 can be combined with BMP4 to commit human pluripotent stem cells to a mesodermal fate.

1. Decursin (Decursinol angelate) is able to attenuate kainic acid-induced seizures and could have potential as an antiepileptic drug. 2. Decursin exhibits hepatoprotective effects , potentially by inhibiting the TGF-β1 induced NOX activation and Smad signaling. 3. Decursin has anti-cancer activity , mediated suppression of the PKCα, MAPK and NF-κB pathways in MCF-7 cells. 4. Decursin exhibits cytotoxicity against various human cancer cells and to possess anti-amnesic activity in vivo through the inhibition of AChE activity.

Isosaponarin is a natural product with multiple activities. It inhibits the increase in Ca2+ levels induced by 4-aminopyridine in rat synaptosomes without affecting the membrane potential of synaptosomes, while reducing the phosphorylation of PKC, PKCα, SNAP-25, and MARCKS, thereby inhibiting the release of glutamate from vesicles in synaptosomes.

pTH-Related Protein (1-40) (human, mouse, rat) enhances calcium absorption in rat intestinal cells by activating the PTHR1 receptor and the PKCα/β signaling pathways. This compound also increases the expression of the parathyroid hormone 1 receptor (PTHR1) and four key proteins involved in transcellular calcium transport: potential vanillin member 6 (TRPV6), calcium-binding protein-D9K (CaBP-D9k), sodium-calcium exchanger 1 (NCX1), and plasma membrane calcium ATPase 1 (PMCA1) [1].

PKCβ inhibitor 1 (KUN79359)(KUN79359) is a potent, selective and ATP-competitive inhibitor of PKC isozymes(IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively).

Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.