s6kinase

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).

FMK is an irreversible inhibitor of RSK2 kinase.

Sodium salicylate (2-Hydroxybenzoic acid sodium salt), a metabolite of acetylsalicylic acid, can inhibit NF-kB and reduce oxidative stress.

CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase/AKT/mTOR pathway and delays sensitive cells in late mitosis.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

Ly-2584702 hydrochloride is a p70S6K selective ATP competitive inhibitor with IC50 of 4 nM.In the S6K1 enzyme assay, the IC50 of LY-2584702 was 2 nM.

MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

BRD7389 is an inhibitor of RSK family kinase with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively.

SL 0101-1 (SL0101) is a selective, efficient, reversible and ATP-competitive inhibitor of p90 ribosomal S6 kinase (RSK) that can permeate cell membranes, with an IC50 value of 89 nM for RSK.SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM. SL 0101-1 (SL0101) is also a potent RSK1/2 inhibitor with a Ki value of 1 μM.

LY-2584702 tosylate salt, a selective ATP-competitive p70S6K inhibitor, is being used in clinical trials for cancer treatment.

Vistusertib (AZD2014) is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.

PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) .In cell-free assays, PF-4708671(PF4708671) is potent for S6K1(Ki50=20 nM, IC50=160 nM).

S6K-18, a highly selective S6K1 inhibitor, inhibits S6K1 with IC50 of 52nM.

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

CHIR-98014 (CT98014) is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.

Quercitrin (3-rhamnosyl quercetin) is a plant-derived flavonoid compound, displays antioxidant and anti-inflammatory activities. Quercitrin can be found in a number of food items such as garden tomato (var. ), German camomile, endive, and kiwi, which makes quercitrin a potential biomarker for the consumption of these food products.

CHIR 98024 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.

GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.

GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

Eudesmin shows antiinflammatory, neuritogenic, anticonvulsant and sedative effects, the mechanism of eudesmin may be related to up-regulation of GABAA and GAD65 expressions, and anti-apoptosis of neuron the in brain.50 microM (+)-eudesmin can induce neurite outgrowth and enhance nerve growth factor (NGF)-mediated neurite outgrowth from PC12 cells by stimulating up-stream MAPK, PKC and PKA pathways.