RET agonist Q525

• CAT Number: I047656
• CAS Number: 2927469-43-8
• Molecular Formula: C16H11ClN2O3
• Molecular Weight: 314.72
• Purity: ≥95%
• IUPAC Name: 7-chloro-6-[4-(hydroxymethyl)anilino]quinoline-5,8-dione
• InChI: InChI=1S/C16H11ClN2O3/c17-12-14(19-10-5-3-9(8-20)4-6-10)15(21)11-2-1-7-18-13(11)16(12)22/h1-7,19-20H,8H2
• SMILES: C1=CC2=C(C(=O)C(=C(C2=O)NC3=CC=C(C=C3)CO)Cl)N=C1

RET agonist Q525 is a highly selective RET agonist which afforded sustained RET activation and prevented photoreceptor neuron loss in the retina. It was active in MG87 RET/GFRa1 cells across a broad range of concentrations and generated large and significant increases in pAkt/pErk. It maintained a high degree of selectivity for RET, because no significant increases in pAkt and pErk were observed in MG87 TrkA cells.
KEYWORDS: RET agonist Q525 | supplier | RET agonist | RET agonist Q 525 | RET agonist Q-525 | CAS [2927469-43-8] | GDNF | RET | agonist | Receptors | Retinitis pigmentosa | Retinal degeneration

Reference

S Jmaeff et al. Small-molecule agonists of the RET receptor tyrosine kinase activate biased trophic signals that are influenced by the presence of GFRa1 co-receptors. J Biol Chem. 2020 May 8;295(19):6532-6542.