CD 2314 is a potent and selective agonist of RARβ with Kd value of 145 and >3760 nM for RARβ and RARα receptors, respectively [1].
Retinoic acid receptor β (RARβ) is a nuclear receptor for retinoic acid and localizes to the cytoplasm and subnuclear compartments. RARβ mediates cellular signalling in cell growth, differentiation and embryonic morphogenesis.
CD 2314 is a potent and selective RARβ agonist. CD 2314 didn’t inhibit the activation-induced apoptosis of thymocytes because of the absent of RARβ in the thymus [1]. CD 2314 inhibited cells growth with IC50 values of 8.0, 3.0, 5.7 and >10 μM for human head and neck squamous cell carcinoma (HNSCC) 22A, 22B, 183A and 886 cell lines, respectively. In UMSCC22B cells, the combination of CD2314 with RXR-selective retinoids, such as SR11234, SR11203, SR11246 and SR11236 inhibited cells growth [2]. In KG-1 cells, CD 2314 didn’t induce folate receptor β (FR-β) expression, indicating that the induction of FR-β was not mediated by RARβ [3].
References:
[1]. Szondy Z, Reichert U, Bernardon JM, et al. Inhibition of activation-induced apoptosis of thymocytes by all-trans- and 9-cis-retinoic acid is mediated via retinoic acid receptor alpha. Biochem J, 1998, 331 ( Pt 3): 767-774.
[2]. Sun SY, Yue P, Mao L, et al. Identification of receptor-selective retinoids that are potent inhibitors of the growth of human head and neck squamous cell carcinoma cells. Clin Cancer Res, 2000, 6(4): 1563-1573.
[3]. Xu Y, Wang T, Tang R, et al. All-trans retinoic acid is capable of inducing folate receptor β expression in KG-1 cells. Tumour Biol, 2010, 31(6): 589-595.