Page last updated: 2024-12-10

fh535

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

FH535: inhibits Wnt signaling [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3463933
CHEMBL ID2363137
CHEBI ID125569
SCHEMBL ID15318105
MeSH IDM0577774

Synonyms (43)

Synonym
CBMICRO_011295
BIM-0011242.P001
STK079761
2,5-dichloro-n-(2-methyl-4-nitrophenyl)benzenesulfonamide
CHEBI:125569
AKOS003980135
CB14399
smsf0005619
FT-0672020
108409-83-2
fh535
n-(2-methyl-4-nitrophenyl)-2,5-dichlorobenzenesulfonamide
beta-catenin/tcf inhibitor, fh535
S7484
BRD-K48112880-001-01-5
CHEMBL2363137 ,
CCG-208119
HY-15721
CS-1538
c13h10cl2n2o4s
SCHEMBL15318105
fh 535
HB0288
AC-31439
DTXSID60392716
Q27216183
J-002138
EX-A388
fh535, >=98% (hplc)
HMS3653N07
fh-535
AS-60177
2,5-dichloro-n-(2-methyl-4-nitrophenyl)benzene-1-sulfonamide
mfcd01212888
SW219729-1
n-[2-methyl-4-nitrophenyl]-2,5-dichlorobenzenesulfonamide
BCP09634
SB19433
2,5-dichloro-n-(2-methyl-4-nitrophenyl)-benzenesulfonamide
nsc-778746
nsc778746
bdbm50509999
beta -catenin/tcf inhibitor, fh535

Research Excerpts

Actions

ExcerptReferenceRelevance
"FH535 was shown to increase CSC-induced cytotoxicity and depress β-catenin expression."( FH535 potentiation of cigarette smoke condensate cytotoxicity is associated with changes in β-catenin and EGR-1 signaling.
Polk, WW,
)
2.3

Compound-Compound Interactions

ExcerptReferenceRelevance
" The purpose of this study was to investigate the inhibitory effect of miR-200a mimics, FH535 combined with taxol on proliferation and invasion of human gastric cancer cell lines SGC-7901 and BGC-823."( Effects of miR-200a and FH535 combined with taxol on proliferation and invasion of gastric cancer.
Du, P; Han, L; Jiang, K; Liu, X; Zhang, A; Zhang, Q, 2018
)
1.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
morphogenesis of an epitheliumNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
cerebrospinal fluid circulationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
renal sodium ion transportNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
plasma membrane organizationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
nuclear migrationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
sensory perception of soundNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of cell population proliferationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
regulation of cell shapeNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
regulation of cell sizeNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
fibroblast migrationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of fibroblast migrationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of sodium ion transportNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
Wnt signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
gland morphogenesisNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
microvillus assemblyNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
actin cytoskeleton organizationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
intracellular phosphate ion homeostasisNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
bile acid secretionNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
glutathione transportNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
positive regulation of monoatomic ion transmembrane transportNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
cilium organizationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
establishment of epithelial cell apical/basal polarityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
maintenance of epithelial cell apical/basal polarityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
regulation of protein kinase activityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of mitotic cell cycleNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
establishment of Golgi localizationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
gamma-aminobutyric acid importNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
auditory receptor cell stereocilium organizationNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
protein-containing complex assemblyNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
renal absorptionNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
protein localization to plasma membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
renal phosphate ion absorptionNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
import across plasma membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
transport across blood-brain barrierNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
regulation of renal phosphate excretionNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid transmembrane transporter activityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
signaling receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
protein bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
beta-catenin bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
chloride channel regulator activityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
phosphatase bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
PDZ domain bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
beta-2 adrenergic receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
type 2 metabotropic glutamate receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
type 3 metabotropic glutamate receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
identical protein bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
transmembrane transporter bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
protein-containing complex bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
myosin II bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
dopamine receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
growth factor receptor bindingNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
channel activator activityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
protein-membrane adaptor activityNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
nucleusNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
plasma membrane protein complexNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
ruffleNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
cytoplasmNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
microvillusNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
endomembrane systemNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
actin cytoskeletonNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
apical plasma membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
filopodiumNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
brush border membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
microvillus membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
vesicleNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
stereocilium tipNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
perinuclear region of cytoplasmNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
extracellular exosomeNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
cell peripheryNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
sperm midpieceNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
apical plasma membraneNa(+)/H(+) exchange regulatory cofactor NHE-RF1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1243334Inhibition of Wnt/beta catenin in human HuH7 cells assessed as decrease in TCF/LEF-dependent promoter activation at 10 uM after 36 hrs by TOPFlash luciferase reporter gene assay relative to control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells.
AID1528297Induction of mitochondrial membrane potential disruption in human DLD1 cells measured after 2 hrs by TMRM staining based fluorescence microscopic analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528286Activation of AMPK in human LS174T cells assessed as reduction in ACC phosphorylation at S79 residue at 3 uM measured within 15 mins by Western blot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528284Inhibition of LiCl-activated Wnt signaling in HEK293 cells at 3 uM by TOPFlash reporter gene assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528287Induction of mitochondrial dysfunction in human DLD1 cells assessed as reduction in mitochondrial ATP production at 3 uM by Seahorse XF real-time assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528299Uncoupling of mitochondrial oxidative phosphorylation in human DLD1 cells at 3 uM in presence of oligomycin A by seahorse XFe96 analyser based assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528291Induction of mitochondrial dysfunction in human LS174T cells assessed as reduction in mitochondrial ATP production at 3 uM by Seahorse XF real-time assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1243332Inhibition of Wnt/beta catenin in human HuH7 cells assessed as [3H]-thymidine incorporation at 10 uM by scintillation counting analysis relative to DMSO-treated control2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells.
AID1528306Uncoupling of mitochondrial oxidative phosphorylation in mouse liver mitochondria assessed as increase in oxygen consumption rate in presence of oligomycin A by seahorse XFe96 analyser based assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1542937Growth inhibition of human SW480 cells expressing NHERF1 incubated for 72 hrs by MTT assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents.
AID1528293Induction of mitochondrial dysfunction in human LS174T cells assessed as increase in glycolytic ATP production at 3 uM by Seahorse XF real-time assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1542936Growth inhibition of human DLD1 cells without NHERF1 expression incubated for 72 hrs by MTT assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents.
AID1528298Induction of mitochondrial membrane potential disruption in human LS174T cells measured after 2 hrs by TMRM staining based fluorescence microscopic analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1542938Inhibition of NHERF1 in human SW620 cells expressing NHERF1 assessed as inhibition cell growth incubated for 72 hrs by MTT assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents.
AID1528285Activation of AMPK in human LS174T cells assessed as increase in AMPK phosphorylation at T172 residue at 3 uM measured within 15 mins by Western blot analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1667214Inhibition of human SET7 overexpressed in Escherichia coli BL21 (DE3) cells at 25 uM preincubated for 15 mins followed by addition of SAM as substrate and biotinylated Histone H3 (1-50) peptide measured after 30 mins by AlphaLISA assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
AID1667215Inhibition of human SET7 overexpressed in Escherichia coli BL21 (DE3) cells at 12.5 uM preincubated for 15 mins followed by addition of SAM as substrate and biotinylated Histone H3 (1-50) peptide measured after 30 mins by AlphaLISA assay relative to contr2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
AID1667213Inhibition of human SET7 overexpressed in Escherichia coli BL21 (DE3) cells at 50 uM preincubated for 15 mins followed by addition of SAM as substrate and biotinylated Histone H3 (1-50) peptide measured after 30 mins by AlphaLISA assay relative to control2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.
AID1528314Inhibition of LiCl-induced Wnt signaling in human LS174T cells assessed as reduction in beta-catenin accumulation2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528289Induction of mitochondrial dysfunction in human DLD1 cells assessed as increase in glycolytic ATP production at 3 uM by Seahorse XF real-time assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
AID1528301Uncoupling of mitochondrial oxidative phosphorylation in human DLD1 cells assessed as increase in oxygen consumption rate at 3 uM in presence of oligomycin A by seahorse XFe96 analyser based assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
An Underlying Mechanism of Dual Wnt Inhibition and AMPK Activation: Mitochondrial Uncouplers Masquerading as Wnt Inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.44)29.6817
2010's36 (87.80)24.3611
2020's4 (9.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.78

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.78 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index6.85 (4.65)
Search Engine Demand Index28.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (2.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other41 (97.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]