CD 161

CD161 is a potent and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 28.2 nM and a Ki of 8.2 nM for BRD4 BD1[1]. CD161 is a C-type lectin-like receptor expressed on the majority of natural killer (NK) cells. CD161 demonstrates high selectivity over 24 non-BET proteins containing bromodomains[2].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

IC50: 28.2 nM (BRD4 BD1)[1]

CD161 has a good pharmacokinetic profile in mice and rats, and demonstrates strong antitumor activity in MV4;11 acute leukemia and MDA-MB-231 breast cancer xenograft models[1].

[1]. Yujun Zhao, et al. Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.J Med Chem. 2018 Jul 26; 61(14): 6110–6120.

[2]. Ayako Kurioka, et al. CD161 Defines a Functionally Distinct Subset of Pro-Inflammatory Natural Killer Cells. Front Immunol. 2018 Apr 9;9:486.