RSK3 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.

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.

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.

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.