2. Academic Validation
  3. Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4

Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4

  • J Med Chem. 2015 Aug 13;58(15):5742-50. doi: 10.1021/acs.jmedchem.5b00226.
Xinlai Cheng 1,  Hiroki Yoshida 1,  Dena Raoofi 1,  Sawsan Saleh 1,  Hamed Alborzinia 1,  Frank Wenke 2,  Axel Göhring 2,  Stefanie Reuter 2,  Nancy Mah 3,  Heiko Fuchs 4,  Miguel A Andrade-Navarro 3,  James Adjaye 4,  Sheraz Gul 5,  Jochen Utikal 6,  Ralf Mrowka 2,  Stefan Wölfl 1
Affiliations

Affiliations

  • 1 †Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Im Neuenheimer Feld 364, D-69120 Heidelberg, Germany.
  • 2 ‡Experimentelle Nephrologie, KIM III, Universitätsklinikum Jena, Am Nonnenplan 2-4, D-07743 Jena, Germany.
  • 3 §Max Delbrück Center for Molecular Medicine, 13125 Berlin, Germany.
  • 4 ∥Institute for Stem Cell Research and Regenerative Medicine, Medical Faculty, Heinrich Heine University, 40225 Duesseldorf, Germany.
  • 5 ⊥European Screening Port GmbH, 22525 Hamburg, Germany.
  • 6 #Skin Cancer Unit, German Cancer Research Center (DKFZ), Heidelberg University, 68167 Mannheim, Germany.
PMID: 26143659 DOI: 10.1021/acs.jmedchem.5b00226
Abstract

The octamer-binding transcription factor 4 (Oct3/4) is a master gene in the transcriptional regulatory network of pluripotent cells. Repression of Oct3/4 in embryonic stem cells (ESCs) is associated with cell differentiation and loss of pluripotency, whereas forced overexpression in cooperation with other transcriptional factors, such as Nanog, Sox2, and Lin28, can reprogram somatic cells back into pluripotent cells, termed induced pluripotent stem cells (iPSCs). However, random integration and potential tumorigenic transformation caused by viral transduction limit the clinical application of iPSCs. By performing a cell-based high throughput screening (HTS) campaign, we identified several potential small molecules as inducers of Oct3/4 expression. Here we report a lead structure ethyl 2-((4-chlorophenyl)amino)-thiazole-4-carboxylate, termed O4I2, showing high activity in enforcing Oct3/4 expression. On the basis of chemical expansion, we further identified derivatives having increased activities toward Oct3/4 induction. Thus, O4I2 and its derivatives should provide a new class of small molecules suitable for iPSC generation.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-18772
    99.30%, Oct3/4 Inducer
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