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O4I1 is a potent Oct3/4 inducer implicated in promoting the expression and stabilization of Oct3/4. O4I1 can enhance the transcriptional activity of Oct3/4 in a variety of human somatic cells. Oct3/4, also known as POU5F1 and Oct4, is a transcription factor which is essential for self-renewal and pluripotency of embryonic stem cells. Oct3/4 is specifically expressed in the ES cells, epiblast, preimplantation embryos, and germ cells, et al [1].

When treated the synthesized cDNA from RNA isolated from the HEK293 cells with 10 μM and 20 μM O4I1 for 72 hrs, the Oct3/4 mRNA levels increased about 2.5- and 4-fold respectively. In human adult primary fibroblast (HF) and human neonatal foreskin fibroblast (HFF) cell lines, treatment with 10 μM O4I1 increased the gene and protein expression level of Oct3/4 after 72 hrs incubation in HF cells and 7 days in HFF cells. The derivatives of O4I1 such as compound 2, showed a time-dependent activation of Oct3/4 and markedly elevated the efficiency of Oct3/4 induction [1].

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