Background:

Target: Oct3; Oct4

IC50: N/A

O4I2, a potent Oct3/4 inducer, is suitable for iPSC generation [1]. The octamer-binding transcription factor 4 (Oct3/4), a member of the POU family of transcription factors, is expressed specifically in pluripotent cells such as induced pluripotent stem cells (iPSCs) and embryonic stem cells (ESCs). Oct3/4 plays a critical role in regulation of the cellular pluripotency core network. The loss-of-function mutation or suppression of Oct3/4 in embryonic stem cells (ESCs) leads to differentiation of ESCs into trophoblast and loss of pluripotency, whereas gain-of-function or forced overexpression Oct3/4, can reprogram somatic cells back into pluripotent stem cells (iPSCs) [1].

In vitro: O4I2 (5, 10, and 20 μM) dose-dependently activated Oct3/4 expression in HEK293 cells, embryonal NCCIT cells, and also in Oct-deficient HeLa cells [1]. In addition, O4I2 (10, and 20 μM) activated Oct3/4 on the transcriptional and translational level in human neonatal foreskin fibroblasts (HFFs), and promoted pluripotency-associated genes (Nanog and Lin28) expression [1].

In vivo: N/A

Reference:
1.  Cheng X, Yoshida H, Raoofi D, Saleh S, Alborzinia H, Wenke F, et al. Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4. J Med Chem. 2015;58(15):5742-50.