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
InChI key
PGOKBMWPBDRDGN-ZXGKGEBGSA-N
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
assay
≥98% (TLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
water: 15 mg/mL, DMSO: 25 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_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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