BIM-46050
BIM-46050 Basic information
- Product Name:
- BIM-46050
- Synonyms:
-
- BIM-46050
- L-Methionine, N-[[(4R)-3-[(2S,3S)-2-[[(2R)-2-amino-3-mercaptopropyl]amino]-3-methylpentyl]-5,5-dimethyl-4-thiazolidinyl]carbonyl]-
- CAS:
- 201487-52-7
- MF:
- C20H40N4O3S3
- MW:
- 480.75
- Mol File:
- 201487-52-7.mol
BIM-46050 Chemical Properties
- Boiling point:
- 699.7±55.0 °C(Predicted)
- Density
- 1.162±0.06 g/cm3(Predicted)
- pka
- 3.32±0.10(Predicted)
BIM-46050 Usage And Synthesis
Description
BIM-46050 is a potent and specific inhibitor of human farnesyltransferase. BIM-46050 is free acidic form of BIM-46068. The IC50 values for in vitro inhibition of human brain FTase indicate that BIM-46050 and the ester form BIM-46068 are potent inhibitors of farnesyltransferase. Their potencies are in the nanomolar range and compare favorably with the compounds B581, FTI-277 and L745,631. B581 is an analog of the tetrapeptide Cys-Val-Phe-Met obtained by replacement of the amino-terminal amide bonds inhibiting processing of farnesylated proteins specifically. FTI-277 is a methyl ester of FTI-276, reported as a preferential inhibitor of FTase over GGTase I (100-fold). L745,631 is a 2-substituted piperazine reported to be a highly selective inhibitor of FTase over GGTase (2,000-fold). The selectivity of BIM-46050 and BIM-46068 for FTase over GGTase is very similar for both compounds (3,000-fold).