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N-[(2S)-((2R)-2-氨基-3-巯基丙基氨基)-3-甲基丁基]-L-苯丙氨酰-L-蛋氨酸

用途

Ftase抑制剂I(B581)是一种有效的、选择性的拟肽法尼基转移酶(Ftase)抑制剂。Ftase抑制剂I对Ftase的选择性高于香叶基香叶基异戊二烯(Ras GG)或脂肪酸肉豆蔻酸酯(Myr Ras)[1]。

名称

[ CAS 号 ]:
149759-96-6

[ 中文名 ]:
N-[(2S)-((2R)-2-氨基-3-巯基丙基氨基)-3-甲基丁基]-L-苯丙氨酰-L-蛋氨酸

[ 英文名 ]:
FTase Inhibitor I

[英文别名 ]:

B581

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 代谢酶/蛋白酶 >> 法呢基转移酶

[体外研究]

Ftase抑制剂I(B581)仅抑制Ras-F转化细胞在软琼脂中生长的能力,但不抑制香叶基基异戊二烯(Ras GG)或脂肪酸肉豆蔻酸酯(Myr-Ras)-(或Raf)转化细胞在软琼脂中生长的能力[1]。

[参考文献]

[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.

物理化学性质

[ 密度 ]:
1.161g/cm3

[ 沸点 ]:
716.1ºC at 760mmHg

[ 分子式 ]:
C₂₂H₃₈N₄O₃S₂

[ 分子量 ]:
470.69

[ 闪点 ]:
386.9ºC

[ 精确质量 ]:
470.23900

[ PSA ]:
180.58000

[ LogP ]:
3.25410

[ 外观性状 ]:
solid | white

[ 蒸汽压 ]:
1.6E-21mmHg at 25°C

[ 折射率 ]:
1.566

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
H2O: soluble

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

文献

[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...

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