staurosporine

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

K-252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi. K-252a inhibits protein kinase (IC50: 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+ calmodulin-dependent kinase type II, and phosphorylase kinase, respectively).

Picroside I (6'-Cinnamoylcatalpol), a hepatoprotective agent, is reported to be antimicrobial and used against hepatitis B. It has antioxidant, and anti-inflammatory activities, it may be the valuable anti-invasive drug candidates for cancer therapy by suppressing Collagenases and Gelatinases. Picroside I can enhance basic fibroblast growth factor(bFGF)-, staurosporine- or dbc-mitogen-activated protein (MAP)-induced neurite outgrowth from PC12D cells.

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

1. Nardosinone has inhibitory effect on Ang II-induced hypertrophy in H9c2 cells, might be mediated by targeting PI3K Akt and MEK ERK signaling pathways. 2. Nardosinone could protect against the neuronal injury exposed to OGD, which may be relevant to the

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

Compound 7, also known as 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine, serves as an inhibitor of protein kinases, displaying IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. Additionally, this compound exhibits significant cytotoxicity towards PC-3 cancer cells, with an IC50 of 0.16 μM [1].