422720
L-744,832
A cell-permeable potent and selective thiol-containing peptidomimetic farnesyltransferase (FTase) inhibitor with anti-tumor properties.
别名:
L-744,832, (2S)-2-[[(2S)-2-[(2S,3S)-2-[(2R)-2-Amino-3-mercaptopropyl]amino]-3-methylpentyl]oxy]-1-oxo-3-phenylpropyl]amino]-4-(methylsulfonyl)-butanoic Acid 1-Methylethyl Ester, L-744,382
质量水平
方案
≥98% (TLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
white
溶解性
water: 15 mg/mL
DMSO: 25 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C26H45N3O6S2/c1-6-19(4)23(28-15-21(27)17-36)16-34-24(14-20-10-8-7-9-11-20)25(30)29-22(12-13-37(5,32)33)26(31)35-18(2)3/h7-11,18-19,21-24,28,36H,6,12-17,27H2,1-5H3,(H,29,30)/t19-,21-,22+,23-,24+/m1/s1
InChI key
PGOKBMWPBDRDGN-ZXGKGEBGSA-N
一般描述
A cell-permeable potent and selective thiol-containing peptidomimetic farnesyltransferase (FTase) inhibitor with anti-tumor properties. Rapidly blocks p70S6K activation and DNA synthesis and promotes apoptosis in transgenic mice. Induces p21 expression and cell cycle arrest in the G1 phase. Displays synergistic effect with paclitaxel and epothilones in inhibiting tumor growth. Also mimics many of the effects of Rapamycin (Cat. No. 553210) and may be effective against tumors that exhibit inappropriate activation of the mTOR/p70S6K pathway.
A potent, cell-permeable, and selective thiol-containing peptidomimetic farnesyltransferase (FTase) inhibitor that blocks p70s6k activation and DNA synthesis and promote apoptosis in transgenic mice. Induces p21 expression and arrests cell in the G1 phase of the cell cycle. Also shown to act synergistically with paclitaxel and epothilones in inhibiting tumor growth and arresting cells in metaphase. Also mimics a number of the effects exhibited by Rapamycin (Cat. No. 553210) and may be effective against tumors that exhibit inappropirate activation of the mTOR/p70s6k pathway in animal models.
生化/生理作用
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
其他说明
Law, B.K., et al. 2000. J. Biol. Chem.275, 10796.
Law, B.K., et al. 1999. J. Biol. Chem.274, 4743.
Barrington, R.E., et al. 1998. Mol. Cell. Biol.18, 85.
Moasser, M.M., et al. 1998. Proc. Natl. Acad. Sci. USA95, 1369.
Sepp-Lorenzino, L., and Rosen, N. 1998. J. Biol. Chem.273, 20243.
Kohl, N.E., et al. 1995. Nat. Med.1, 792.
Sepp-Lorenzino, L., et al. 1995. Cancer Res.55, 5302.
Law, B.K., et al. 1999. J. Biol. Chem.274, 4743.
Barrington, R.E., et al. 1998. Mol. Cell. Biol.18, 85.
Moasser, M.M., et al. 1998. Proc. Natl. Acad. Sci. USA95, 1369.
Sepp-Lorenzino, L., and Rosen, N. 1998. J. Biol. Chem.273, 20243.
Kohl, N.E., et al. 1995. Nat. Med.1, 792.
Sepp-Lorenzino, L., et al. 1995. Cancer Res.55, 5302.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Eugènia Almacellas et al.
Autophagy, 17(3), 796-813 (2020-06-24)
Lysosomes, as primary degradative organelles, are the endpoint of different converging pathways, including macroautophagy. To date, lysosome degradative function has been mainly studied in interphase cells, while their role during mitosis remains controversial. Mitosis dictates the faithful transmission of genetic
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