General
Preferred name
EF24
Synonyms
EF 24 ()
EF-24 ()
3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone ()
P&D ID
PD041146
CAS
342808-40-6
Tags
available
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 ¦ÌM and 0.8 ¦ÌM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK[1][2][3][4].
PRICE 91
DESCRIPTION EF24 (3,5-Bis[(2-fluorophenyl)Methylene]-4-piperidinone) treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK. EF24 shows potent anti-tumor activity in oral squamous cell carcinoma (OSCC) via deactivation of the MAPK/ERK signaling pathway. (TargetMol Bioactive Compound Library)
Cell lines
22
Organisms
3
Compound Sets
3
MedChem Express Bioactive Compound Library
HY-119272
TargetMol Bioactive Compound Library
T27242
ZINC Tool Compounds
ZINC000034009101
External IDs
11
Properties
(calculated by RDKit )
Molecular Weight
311.11
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
2
Ring Count
3
Aromatic Ring Count
2
cLogP
3.6
TPSA
29.1
Fraction CSP3
0.11
Chiral centers
0.0
Largest ring
6.0
QED
0.86
Structural alerts
1
ene_one_ene_A(57)
[#6]=!@[#6](-[!#1])-@[#6](=!@[!#6&!#1])-@[#6](=!@[#6])-[!#1]
PAINS Family B
Custom attributes
(extracted from source data)
Target
Apoptosis
Caspase
ERK
NF-κB
p38 MAPK
Reactive Oxygen Species (ROS)
caspase-3
Caspase-9
MEK1
Reactive Oxygen Species
Pathway
Immunology/Inflammation
MAPK/ERK Pathway
Metabolic Enzyme/Protease
Stem Cell/Wnt
MAPK
Proteases/Proteasome
NF-¦ÊB
Source data