RIOK2-IN-1

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].

Product Specifications

CAS Number

[1088216-72-1]

UNSPSC

12352005

Hazard Statement

H302-H315-H319

Target

Ser/Thr Kinase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/riok2-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C(CC1=CC2=C(C=CC=C2)C=C1)NC3=NC=CC(C)=C3

Molecular Formula

C18H16N2O

Molecular Weight

276.33

Precautions

P264-P270-P280-P302+P352-P305+P351+P338-P330-P362+P364-P501

References & Citations

[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.