RIO Kinase
Rright open reading frame Kinase
RIO kinase (RIOK) are a class of highly conserved atypical serine/threonine kinases, mainly including RIOK1, RIOK2, and RIOK3. RIOK possess both kinase and ATPase characteristics, and their core functions primarily involve the maturation of the pre-40S ribosomal small subunit, 18S rRNA processing, and ribosome biogenesis, thereby maintaining protein translation capacity and cell proliferation.
RIOK are not only ribosome assembly factors but also crucial nodes connecting the translation system and oncogenic signaling. RIOK1/2 can enhance ribosome production, protein translation, and AKT/mTOR signaling output, promoting cell proliferation, EMT, and tumor progression; RIOK3 participates in the TBK1-IRF3-IFN and NF-κB pathways, regulating innate immune and inflammatory responses. Due to the high dependence of cancer cells on ribosome production and translation capacity, RIOK have become an emerging anticancer target.
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RIO Kinase Related Products (8)
Related Products (8)
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NSC139021
0 ImagesNSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling.
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ERGi-USU-6 mesylate
0 ImagesCat. No.: HY-139893CAS No.: 2756327-67-8ERGi-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.
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CQ627
0 ImagesCQ627 is a molecular glue degrader of right open reading frame kinase 2 (RIOK2). CQ627 inhibits the ATPase activity of RIOK2 in MOLT-4 cells with an IC50 of 98 nM. By recruiting the E3 ubiquitin ligase RNF126, CQ627 promotes RIOK2 ubiquitination and induces its degradation via the ubiquitin-proteasome system (UPS), while inhibiting RIOK2-dependent mTOR/AKT signaling, suppressing cancer cell proliferation, and inducing G2/M cell cycle arrest and apoptosis. CQ627 can be used in studies related to RIOK2-targeted protein degradation and leukemia.
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TIBI
0 ImagesTIBI is a potent and ATP-competitive inhibitor of Rio1 (IC50: 0.09 μM, Ki: 0.05 μM). TIBI enhances the thermostability of the enzyme Rio1.
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CQ3196
0 ImagesCat. No.: HY-175733CAS No.: 3105591-09-8CQ3196 is an orally active RIOK2 inhibitor with a Kd 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.
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RIOK2-IN-1
0 ImagesCat. No.: HY-156792CAS No.: 1088216-72-1RIOK2-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.
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RIOK2-IN-2
0 ImagesCat. No.: HY-156465CAS No.: 2648987-17-9RIOK2-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.
