rsk1

RSK-IN-1 (compound 7d) shows anti-tumor activity. RSK-IN-1 is an inhibitor of RSK that inhibits the phosphorylation of YB-1 [1].

BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31/24/18/15 nM for RSK1/2/3/4).

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.

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.

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

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).

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.

Hu7691 free base is an orally active, potent and selective Akt inhibitor with anti-proliferative and neurogenic effects on a variety of neuroblastoma cell lines.Hu7691 free base inhibits Akt1, Akt2, and Akt3 and induces differentiation of neuroblastoma cells.

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.

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.

GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties.

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.

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.

Hu7691 is an orally active, selective and potent Akt inhibitor that inhibits Akt1, Akt2 and Akt3, inhibits proliferation of neuroblastoma cells and induces differentiation of neuroblastoma cells.

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.

DTS is a selective and isoform-specific RSK1 kinase inhibitor. It also has broad cancer therapeutic potential.

c-Ceritinib TFA salt is a coupleable ceritinib analog with a linker which also binds multiple other kinases, including FAK1, RSK1/2, ERK1/2, CAMKK2 and FER.

Prexasertib dimesylate (LY2606368 dimesylate) is a highly selective ATP-competitive second-generation inhibitor of checkpoint kinase 1 (CHK1). With a K i of 0.9 nM and an IC 50 of <1 nM, Prexasertib dimesylate effectively inhibits CHK2 (IC 50 = 8 nM) and RSK1 (IC 50 = 9 nM). Its mechanism of action involves inducing double-stranded DNA breakage and replication catastrophe, ultimately leading to apoptosis. Moreover, Prexasertib dimesylate demonstrates potent anti-tumor activity.

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

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is an ATP-competitive, selective, second generation cell cycle detection site kinase 1 (CHK1) inhibitor (IC50<1 nM, Ki: 0.9 nM). Prexasertib Mesylate Hydrate inhibits CHK2 (IC50: 8 nM) and RSK1 (IC50: 9 nM). prexasertib Mesylate Hydrate causes double-stranded DNA breaks and replication mutations, induces apoptosis and exhibits potent anti-tumour effects.

AKT-IN-2 is a selective, and orally bioavailable AKT inhibitor (IC50: 5 nM for AKT1).

AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.