RSK2 Inhibitor

BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.

Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC₅₀ of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a K_i of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC₅₀s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation.

Pluripotin is a dual inhibitor of ERK1 and RasGAP with K_Ds of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC₅₀s of 0.5, 2.5, 3.3, and 10.0 μM, respectively.

FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.

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

CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.

BRD7389 is a specific RSK family kinase inhibitor with IC₅₀s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells.

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

RSK-IN-2 (Compound 3e) is a RSK inhibitor, with IC₅₀ s of 37.89 nM (RSK2), 30.78 nM (RSK1), 20.51 nM (RSK3), 91.28 nM (RSK4). RSK-IN-2 inhibits tumor cell proliferation, induces apoptosis and causes cell cycle arrest in the G2/M phase.

RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3.

RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma.

RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase.

(E/Z)-PV1162 is an inhibitor of Chk2 and RSK2. (E/Z)-PV1162 regulates the ATM-Chk2 pathway, apoptosis, cell cycle regulation and hypoxia-related processes. (E/Z)-PV1162 is applicable for cancer research.