| Identification | Back Directory | [Name]
RO 08-2750 | [CAS]
37854-59-4 | [Synonyms]
RO 08-2750
7,10-DIMETHYL-2,4-DIOXOBENZO[G]PTERIDINE-8-CARBALDEHYDE
2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde
Benzo[g]pteridine-8-carboxaldehyde, 2,3,4,10-tetrahydro-7,10-dimethyl-2,4-dioxo- | [Molecular Formula]
C13H10N4O3 | [MDL Number]
MFCD09038552 | [MOL File]
37854-59-4.mol | [Molecular Weight]
270.24 |
| Hazard Information | Back Directory | [Uses]
Ro 08-2750 is a TrkA inhibitor and NGF-induced apoptosis inhibitor. | [Definition]
ChEBI: 7,10-dimethyl-2,4-dioxo-8-benzo[g]pteridinecarboxaldehyde is a flavin. | [Biological Activity]
Non-peptide inhibitor of NGF that binds the NGF dimer (K D ~ 1 μ M) possibly causing a conformational change. Inhibits binding selectively to p75 NTR at submicromolar concentrations and to both p75 NTR and TrkA at higher concentrations (> 5 μ M). Prevents NGF-induced apoptosis in SK-N-MC cells. | [in vitro]
ro 08-2750 can bind to the ngf dimer with ~ 1:1 binding ratio. binding of ro 08-2750 to ngf induces ngf a concentration-dependent conformational change [1]. binding with low concentration of ro 08-2750, ngf can no longer bind to p75ntr anymore, however, binding to trka is not impaired. at higher concentrations of ro 08-2750 more than 5 mm, the ngf/ro 08-2750 complex can not bind to trka as well. in sk-n-mc cells, ro 08-2750 leads to inhibition of ngf-induced programmed cell death. in pc12 cells, ro 08-2750 can enhance the signal pathway through trka[2]. | [IC 50]
1 μm (binds to ngf) [1] | [storage]
Store at -20°C | [References]
[1] arkin mr, wells ja. small-molecule inhibitors of protein-protein interactions: progressing towards the dream. nat rev drug discov. 2004 apr;3(4):301-17.
[2] niederhauser o, mangold m, schubenel r, kusznir ea, schmidt d, hertel c. ngf ligand alters ngf signaling via p75(ntr) and trka. j neurosci res. 2000 aug 1;61(3):263-72. |
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