BMS961 is a potent and selective retinoic acid receptor gamma (RARγ) agonist with IC50 values of 30 nM.
RARγ belongs to the family of nuclear receptors which regulates transcription. RARγ mediates the anti-proliferative and apoptotic effects of retinoids in cancer cells such as neuroblastoma cells. RARγ is the principal receptor that regulates RA mediated growth arrest in keratinocytes.
In vitro, application of BMS961on mouse ear skin was found to cause a significant increase of thymic stromal lymphopoietin (TSLP) transcripts1. In addition, exposure of BMS861 on limbs at low concentration leads to retarded growth of the zeugopod (long bones) and intactness of autopod (paw). However, high concentration of BMS961treatment caused equal undifferentiation of both limb regions 2.
In WT mice, RARγ agonists BMS961treatment resulted in an increase of the ear TSLP transcripts and serum TSLP, which indicates an involvement of RAR-mediated events in transcriptional activation of TSLP expression1.
References:
1. Li M, Hener P, Zhang Z, et al. Topical vitamin D3 and low-calcemic analogs induce thymic stromal lymphopoietin in mouse keratinocytes and trigger an atopic dermatitis. Proceedings of the National Academy of Sciences of the United States of America. 2006;103(31):11736-11741.
2. Galdones E, Hales BF. Retinoic acid receptor gamma-induced misregulation of chondrogenesis in the murine limb bud in vitro. Toxicological sciences : an official journal of the Society of Toxicology. 2008;106(1):223-232.