RIO Kinase Inhibitor

CQ211 is a potent and selective RIOK2 inhibitor with a K_d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines.

ERGi-USU-6 mesylate (Compound 7b) is an inhibitor of ERG and RIOK2 (IC₅₀ values: 0.17 and 0.13 μM in VCaP cells, respectively). ERGi-USU-6 mesylate exhibits anticancer activity against ERG-positive prostate cancer.

TIBI is a potent and ATP-competitive inhibitor of Rio1 (IC₅₀: 0.09 μM, K_i: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1.

CQ3196 is an orally active RIOK2 inhibitor with a K_d of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC₅₀ value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research.

RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.

RIOK2-IN-2 (8) is a RIOK2 inhibitor, with IC₅₀ values of 3.02 μM and 5.34 μM in MKN-1 and MOLT4 cells, respectively.