480150-M
Ras-Net (Elk-3) Pathway Inhibitor, XRP44X
The Ras-Net (Elk-3) Pathway Inhibitor, XRP44X, also referenced under CAS 729605-21-4, controls the biological activity of Ras-Net (Elk-3).
别名:
Ras-Net (Elk-3) Pathway Inhibitor, XRP44X, Actin Assembly Inhibitor XVI, Ras Activation Inhibitor, Tubulin Polymerization Inhibitor IX, 1-(3-Chlorophenyl)-4-((3-methyl-1-phenyl-1H-pyrazol-5-yl)carbonyl)piperazine
InChI
1S/C21H21ClN4O/c1-16-14-20(26(23-16)18-7-3-2-4-8-18)21(27)25-12-10-24(11-13-25)19-9-5-6-17(22)15-19/h2-9,14-15H,10-13H2,1H3
InChI key
NPHPNBGYPKBDDB-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mM, ethanol: 50 mM
General description
A cell-permeable pyrazole compound that is shown to prevent in vitro tubulin polymerization (IC50 = 0.2 µM) by targeting Colchicine (Cat. No. 234115 ) binding site (Kd = 0.3 µM) in cell-free assays and induce blebs formation in HUVEC cultures by perturbing both tubulin microtubles and actin cytoskeleton structures. Unrelated to its effects on actin and tubulin filaments, XRP44X is also reported to block the activations of Ras and its downstream effector molecules, such as Raf, MEK, Erk, Rsk, and Net (Elk-3/SAP-2/Erp), upon FGF-2 (Cat. No. 341595 ) stimulation. Potently inhibits the growth of HUVEC, NIH3T3, as well as 9 other cancer cell lines in antiproliferation assays (IC50 ≤11.3 nM).
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wasylyk, C., et al. 2008. Cancer Res.68, 1275.
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 3
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