CYT997
CAS No. | 917111-44-5 | Cat. No. | BCP02278 |
Name | CYT997 | ||
Synonyms | CYT-997;CYT 997;Lexibulin; | ||
Formula | C24H30N6O2 | M. Wt | 434.53 |
Description | CYT997 (1 μM) treatment for 24 hours in A549 cells induces rapid reorganization of microtubules including the destruction of the existing microtubule network and accumulation of tubulin in plaques within the cytoplasm of some cells, leading to significant cell morphology alterations including the loss of adhesion and cell rounding. CYT997 displays potent cytotoxic activity against a range of 16 cancer cells with IC50 ranging from 9 nM for HepG2 to 101 nM for KHOS/NP. Especially, CYT997 exhibits potent activity against HCT15 cells, known to possess the multidrug resistance mechanism Pgp (MDR+), with IC50 of 52 nM. Through inhibition of microtubule polymerization, CYT997 blocks the cell cycle at the G2-M boundary, and induces an increase in phosphorylated Bcl-2 and increased expression of cyclin B1, as well as caspase-3 activation and the generation of poly (ADP-ribose) polymerase. CYT997 treatment causes a rapid and reversible increase in the permeability of HUVEC monolayers with IC50 o | ||
Pathways | Cell Cycle/DNA Damage | ||
Targets | Microtubule |
Structure
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