| Description | Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM. Ro 08-2750 inhibits NGF binding to p75NTR selectively over TRKA. |
| In vitro | Ro 08-2750 inhibits the survival of human AML lines and patient cells. Ro 08-2750 suppresses MSI2 RNA-binding and alters the MSI2 gene signature. Ro 08-2750 binds to the NGF dimer thereby probably inducing a change in its conformation such that NGF cannot bind to p75NTR anymore. Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis in myeloid leukemia cells. Ro 08-2750 (10 nM) fully rescues cells from undergoing NGF-induced SK-N-MC 103 cell death [2][3]. |
| In vivo | In a myeloid leukemia model in vivo, Ro 08-2750 (13.75 mg/kg; i.p.) suppresses leukemogenesis [3]. |
| Target activity | NGF:~1 μM |
| molecular weight | 270.24 |
| Molecular formula | C13H10N4O3 |
| CAS | 37854-59-4 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 3.5 mg/mL (12.95 mM), Sonication and heating to 80℃ are recommended. |
| References | 1. Arkin MR, et al. Small-molecule inhibitors of protein-protein interactions: progressing towards the dream. Nat Rev Drug Discov. 2004 Apr;3(4):301-17. 2. Niederhauser O, et al. NGF ligand alters NGF signaling via p75(NTR) and trkA. J Neurosci Res. 2000 Aug 1;61(3):263-72. 3. Minuesa G, et al. Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia. Nat Commun. 2019 Jun 19;10(1):2691. |