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| | RO 08-2750 Basic information |
| Product Name: | RO 08-2750 | | Synonyms: | 2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde;RO 08-2750;7,10-DIMETHYL-2,4-DIOXOBENZO[G]PTERIDINE-8-CARBALDEHYDE;Benzo[g]pteridine-8-carboxaldehyde, 2,3,4,10-tetrahydro-7,10-dimethyl-2,4-dioxo-;growth,MSI,Ro 082750,p75NTR,TRKA,RNA-binding,Nerve,NGF,Inhibitor,leukemia,Apoptosis,AML,Ro 08-2750,inhibit,Ro 08 2750,factor,MUSASHI;7,10-dimethyl-2,4-dioxo-2,3,4,10-tetrahydrobenzo[g]pteridine-8-carbaldehyde | | CAS: | 37854-59-4 | | MF: | C13H10N4O3 | | MW: | 270.24 | | EINECS: | | | Product Categories: | | | Mol File: | 37854-59-4.mol |  |
| | RO 08-2750 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | ≤2.7mg/ml in DMSO | | form | solid | | color | Orange |
| | RO 08-2750 Usage And Synthesis |
| 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. |
| | RO 08-2750 Preparation Products And Raw materials |
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