RSK4 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.

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.

RSK4-IN-1 is a potent RSK4 inhibitor with a IC₅₀ value of 9.5 nM. RSK4-IN-1 has antitumor activity.

RSK4-IN-1 TFA is a potent RSK4 inhibitor with a IC₅₀ value of 9.5 nM. RSK4-IN-1 TFA has antitumor activity.

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.

RSK4-IN-2 (compound 16o) is a potent, orally active RSK4 inhibitor with an IC₅₀ of 17 nM. RSK4-IN-2 suppresses esophageal squamous cell carcinoma (ESCC) cell growth and invasion, by inhibiting phosphorylation of RSK4 downstream targets. RSK4-IN-2 inhibits tumor growth and metastasis in ESCC mouse models. RSK4-IN-2 can be used for ESCC research.