CpdA

CpdA is a non-steroidal selective glucocorticoid receptor modulator.¹ It is an aziridine precursor that can infiltrate cells and is translocated to the nucleus.^1,2 It inhibits glucocorticoid receptor dimerization, which prevents transcription of gene targets such as NF-κB and subsequent cytokines through transrepression.³ Studies have shown contradictory results for binding affinity of CpdA compared with dexamethasone (Item No. 11015) that were either higher (4-fold, IC₅₀ = 6.4 nM and 25.9 nM, respectively, in L929sA cells) or lower (63-fold, K_d = 81.8 nM and 1.29 nM, respectively, in BWTG3 cells) in whole cell binding assays.^2,3

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1. Lesovaya, E., Yemelyanov, A., Swart, A.C., et al. Discovery of Compound A - a selective activator of the glucocorticoid receptor with anti-inflammatory and anti-cancer activity. Oncotarget 6(31), 30730-30744 (2015).

2. De Bosscher, K., Vanden Berghe, W., Beck, I.M., et al. A fully dissociated compound of plant origin for inflammatory gene repression. Proc. Natl. Acad. Sci. USA 102(44), 15827-15832 (2005).

3. Robertson, S., Allie-Reid, F., Vanden Berghe, W., et al. Abrogation of glucocorticoid receptor dimerization correlates with dissociated glucocorticoid behavior of compound a. The Journal of Biological Chemisty 285(11), 8061-8075 (2010).