Drug intelligence / Profile preview

RepSox

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

RepSox (also known as E-616452 or SJN 2511) is a potent, selective, and cell-permeable small molecule inhibitor of the transforming growth factor-beta (TGF-β) type I receptor, also known as activin receptor-like kinase 5 (ALK5). It was originally identified by GlaxoSmithKline and later named RepSox (Replacement of Sox2) by researchers at the Harvard Stem Cell Institute after discovering its ability to replace the transcription factor Sox2 during the reprogramming of somatic cells into induced pluripotent stem cells (iPSCs). RepSox works by selectively inhibiting ALK5 autophosphorylation and blocking downstream TGF-β/Smad signaling, which in turn induces the expression of Nanog. It is widely used as a research tool in stem cell biology, regenerative medicine, oncology, and metabolic disease research.

Other names
2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine2-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]-1,5-naphthyridineALK5 Inhibitor IIALK-5 Inhibitor IIALK 5 Inhibitor II
02

Targets

TGFBR1

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