ribosomal s6 kinase (rsk)

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).

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

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

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).

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.

FMK-MEA is a potent and selective inhibitor of p90 Ribosomal S6 Kinase (RSK).

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.

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

Carnosol is an Nrf2 activator, increasing Nrf2 levels and promoting heme oxygenase 1 (HMOX1) expression. It is a ribosomal S6 kinase (RSK2) inhibitor and can be used in gastric cancer-related research with an IC50 value of approximately 5.5 μM.

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.

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.

DD1 (HUN85111) is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.

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.

Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.

LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM).

Bisindolylmaleimide V, a bisindolylmaleimide derivative, is an inactive of a kinase inhibitor.

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.

LJH685 is an effective pan-RSK inhibitor for RSK1 2 3 (IC50: 6 5 4 nM).