RepSox
Chemical compound
From Wikipedia, the free encyclopedia
RepSox is a small molecule inhibitor of TGFβR1,[1][2] also known as ALK5. As a mimetic of the effects of the SOX2 protein, it has gained attention in the fields of stem cell research and regenerative medicine.
| |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| ATC code |
|
| Legal status | |
| Legal status |
|
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.190.188 |
| Chemical and physical data | |
| Formula | C17H13N5 |
| Molar mass | 287.326 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
It was identified after the discovery of the Yamanaka factors.[3] It has shown promise in a variety of in-vitro and in-vivo rodent trials modelling various diseases. It inhibits TGFβR1 autophosphorylation by preventing the protein from binding with ATP, inhibits the binding of TGF-β to TGFβR1, and prevents the transcription of genes activated by TGFβR1 with nanomolar potency.[4] RepSox is a member of the 1,5-naphthyridine class.
Research
In an in-vivo trial of rats with ovariectomy-induced osteoporosis, RepSox was shown to prevent bone loss.[1] RepSox is included as a part of some chemical cocktails intended for cellular reprogramming and anti-aging,[5] where it works by inducing the expression of the gene Nanog.[6]
RepSox suppresses the proliferation of osteosarcoma cells via suppression of the JNK/Smad3 signalling pathway, and was able to induce cell cycle arrest, promote apoptosis and prevent migration of the cancer cells. The results were replicated both in-vitro and in-vivo.[7]
RepSox was able to promote the transformation of glial cells to neurons in the enteric nervous system of adult mice, consequently influencing gastrointestinal motility, and underlining a potential therapeutic use of RepSox in enteric neuropathies.[8]
History
RepSox was discovered by a team at the Harvard Stem Cell Institute looking for way to induce pluripotency without inserting the gene Sox2 into cells. They discovered a molecule which was capable of this but also was able to reprogram cells in the absence of c-Myc, a tumour promoting gene. They named the molecule RepSox since it can replace Sox2 and in homage to the Boston Red Sox.[3]