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Molecular inhibitor series

PLX8394 CAS:1393466-87-9

Release time:2017/06/20 Click rate:

PLX8394 is a potent and selective inhibitor of B-RafV600E (IC50~5 nM).

IC50 value: ~5 nM
Target: B-RafV600E
in vitro: PLX8394 potently inhibits phosphorylation of ERK1/2 in PRT #3 and PRT #4 cells in addition to parental cells. PLX8394 potently inhibits ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX8394 effectively reducs cyclin D3 and cyclin D1, phosphorylation of retinoblastoma protein, and expression of cyclin A2 in parental cells. PLX8394 reduces levels of these cell cycle markers in PRT #3 and PRT #4 cells. Consistent with these effects, PLX8394 inhibits EdU incorporation into PRT #3 and PRT #4 cells in S phase entry assays. PLX8394 inhibits ERK1/2 phosphorylation and the growth of vemurafenib-resistant cells harboring either a BRAF V600K/L505H double mutation or an transposon-induced, N-terminal truncated form of BRAF

PLX8394 Basic information

Product Name: PLX8394
Synonyms: PLX8394
CAS: 1393466-87-9
MF:  
MW: 0
EINECS:  
Product Categories:  
Mol File: Mol File