s6 kinase

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).

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

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.

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

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.

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.

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM, 28-fold greater selectivity for Akt2 than the closely related PKA kinase.

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).

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

Pluripotin (SC1) (SC1), which keep embryonic stem cell (ESC) self-renewal, is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP.

AT7867 is a potent ATP-competitive inhibitor of Akt1 2 3 and p70S6K PKA with IC50 values of 32 nM, 17 nM, 47 nM, 85 nM, and 20 nM, respectively, exhibiting little activity outside the AGC kinase family.

S6 Kinase Substrate Peptide (32) is a peptide utilized to measure the activity of kinases that phosphorylate ribosomal protein S6, and it can also serve as a substrate.

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.

FMK is an irreversible inhibitor of RSK2 kinase.

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

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

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.

BI-D1870 is a highly specific, blood-brain-permeable, and ATP-competitive inhibitor of the N-terminal AGC kinase domain of RSK, with IC50 values ​​of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4.

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.

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.

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