| Bioactivity | 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[1]. |
| Name | RIOK2-IN-1 |
| CAS | 1088216-72-1 |
| Formula | C18H16N2O |
| Molar Mass | 276.33 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ouyang Y, et al. Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro-4H-[1,2,3]triazolo[4,5-c]quinolin-4-one (CQ211) as a Highly Potent and Selective RIOK2 Inhibitor. J Med Chem. 2022 Jun 9;65(11):7833-7842. |
RIOK2-IN-1
CAS: 1088216-72-1 F: C18H16N2O W: 276.33
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM)
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