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Description: QL-47 (also known as QL-XII-47) is a novel, potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM. QL47 acts by covalently modifying Cys481 of BTK. QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCgamma2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest which is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations.
References: ACS Chem Biol, 2014.
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