FTase Inhibitor I

Names

[ Name ]:
FTase Inhibitor I

[Synonym ]:
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-amino-3-sulfanylpropyl]amino]-3-methylbutyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoic acid
B581

Biological Activity

[Description]:

Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Farnesyl Transferase

[In Vitro]

Ftase inhibitor I (B581) inhibits the ability of only Ras-F-transformed cells, but not geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras)- (or Raf-) transformed cells, to grow in soft agar[1].

[References]

[1]. A D Cox, et al. The CAAX peptidomimetic compound B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation. J Biol Chem. 1994 Jul 29;269(30):19203-6.

Chemical & Physical Properties

[ Density]:
1.161g/cm3

[ Boiling Point ]:
716.1ºC at 760mmHg

[ Molecular Formula ]:
C₂₂H₃₈N₄O₃S₂

[ Molecular Weight ]:
470.69

[ Flash Point ]:
386.9ºC

[ Exact Mass ]:
470.23900

[ PSA ]:
180.58000

[ LogP ]:
3.25410

[ Appearance of Characters ]:
solid | white

[ Vapour Pressure ]:
1.6E-21mmHg at 25°C

[ Index of Refraction ]:
1.566

[ Storage condition ]:
−20°C

[ Water Solubility ]:
H2O: soluble

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S22-S24/25

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

[Anti tumor activity of farnesyl transferase inhibitor].

Gan To Kagaku Ryoho. 24(2) , 145-55, (1997)

Posttranslational farnesylation by farnesyltransferase (FTase) is critical for the function of ras oncogene product and FTase has attracted attention as the new target of anticancer agents. B956 and B...

Bcl-2 differentially targets K-, N-, and H-Ras to mitochondria in IL-2 supplemented or deprived cells: implications in prevention of apoptosis.

Oncogene 18(35) , 4930-9, (1999)

IL-2 deprivation triggers apoptosis in the murine T cell line TS1alphabeta, a process that can be blocked by overexpression of Bcl-2. Here we show that Bcl-2 and Ras proteins interact in mitochondria ...

Peptidomimetic inhibitors of Ras farnesylation and function in whole cells.

J. Biol. Chem. 268(25) , 18415-8, (1993)

The ras protooncogene is involved in regulation of cell growth. Mutations that activate the protein result in uncontrolled cell growth. Ras undergoes a series of posttranslational processing events, t...

Related Compounds

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