SB 4

BMP signaling agonist sb4 is a small molecule BMP signaling agonist with EC50 of 73.6 nM, enhances the efficacy of BMPs and activates endogenous BMP4 target genes; increases the phosphorylation of key second messengers (SMADs-1/5/9) and also increased expression of direct target genes (inhibitors of DNA binding, ID1 and ID3) in canonical BMP signaling.

Research Areas >> Cancer

IC50: BMP4 signal[1]

BMP signaling agonist sb4 (0.05 μM-1 μM; 24 hours) induces phosphorylated SMAD-1/5/9 in a dose-dependent manner in PRECs cells under serum-starved conitions[1]. BMP signaling agonist sb4 (1 μM; 0-60 mins) enhances the efficacy of signaling at each concentration of rhBMP4 tested. This effect is most pronounced at low concentrations of rhBMP4, whereby sb4 increases BRE-luc expression 2-fold at 0.4 ng/ml of rhBMP4[1]. Western Blot Analysis[1] Cell Line: Primary mouse kidney epithelial cells (PRECs) Concentration: 0.05 μM-1 μM Incubation Time: 24 hours Result: Incresed p-SMAD-1/5/9 abundance in PRECs. Western Blot Analysis[1] Cell Line: BRE-Luc cells Concentration: 1 μM Incubation Time: 0min, 5 mins, 15 mins, 30 mins, 45 mins, 60 mins Result: Acted to stabilize p-SMAD-1/5/9 to enhance the transcriptional response.

[1]. Bradford STJ, et al. High-throughput screens for agonists of bone morphogenetic protein (BMP) signaling identify potent benzoxazole compounds.J Biol Chem. 2019 Mar 1;294(9):3125-3136.