Page last updated: 2024-08-02 18:43:27

wp1066

Description

Cross-References

ID SourceID
PubMed CID11210478
CHEMBL ID1923234
SCHEMBL ID1315831
SCHEMBL ID1315826
MeSH IDM0509983

Synonyms (32)

Synonym
wp1066 ,
SCHEMBL1315831
SCHEMBL1315826
wp-1066
857064-38-1
(s,e)-3-(6-bromopyridin-2-yl)-2-cyano-n-(1-phenylethyl)acrylamide
AKOS016007983
wp 1066
BCP0726000087
CHEMBL1923234
wp1066/wp-1066
2-propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-n-((1s)-1-phenylethyl)-, (2e)-
unii-63v8aie65t
63v8aie65t ,
gtpl7972
HY-15312
MLS006010178
smr004701286
DTXSID50235007
AC-28413
mfcd12912450
EX-A760
SW219153-1
wp1066stat inhibitor iii
DB12679
bdbm50557738
S2796
Q27089227
AS-19242
CCG-268106
stat3 inhibitor iii, wp1066
A863463

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency10.4353AID1347411
Interferon betaHomo sapiens (human)Potency10.4353AID1347411

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Signal transducer and activator of transcription 3Homo sapiens (human)IC502.1450AID1709758; AID1709794

Bioassays (20)

Assay IDTitleYearJournalArticle
AID1709760Cytotoxicity against human HEK 293T cells assessed as cell growth inhibition at 50 uM measured after 48 hrs by MTT assay2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID632967Antitumor activity against human U266 cells after 24 to 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1768839Cytotoxicity against human HCCLM3 cells assessed as cell viability up to 50 uM measured upto 72 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 10-15, Volume: 50ISSN: 1464-3405Pyrimidine-2,4-dione targets STAT3 signaling pathway to induce cytotoxicity in hepatocellular carcinoma cells.
AID1768838Cytotoxicity against human HepG2 cells assessed as cell viability up to 50 uM measured upto 72 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 10-15, Volume: 50ISSN: 1464-3405Pyrimidine-2,4-dione targets STAT3 signaling pathway to induce cytotoxicity in hepatocellular carcinoma cells.
AID632968Antitumor activity against human MM1 cells after 24 to 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID632966Antitumor activity against human OCI-My4 cells after 24 to 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1709759Cytotoxicity against human HeLa cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID1709758Inhibition of IL-6 induced STAT3 transcriptional activity in human HEK-Blue IL-6 cells assessed as secreted embryonic alkaline phosphatase reporter gene expression measured after 20 hrs by microplate reader2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID632964Antitumor activity against human U373MG cells after 24 to 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1709807Cytotoxicity against human HEK-Blue IL-6 cells assessed as cell death at > 10 uM2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID632970Ratio of AG490 IC50 to compound IC50 for human U373MG cells2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1064868Cytotoxicity against human 73M cells assessed as cell viability after 8 days by Alamar Blue assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
ISSN: 1948-5875
Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.
AID1709794Inhibition of IL-6 induced STAT3 transcriptional activity in human HEK-Blue IL-6 cells assessed as secreted embryonic alkaline phosphatase reporter gene expression by microplate reader2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID632965Antitumor activity against human U87MG cells after 24 to 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1709761Cytotoxicity against human HEK 293T cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by MTT assay2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
ISSN: 1948-5875
AID632969Ratio of AG490 IC50 to compound IC50 for human U87MG cells2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
ISSN: 1464-3391
Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.
AID1064870Cytotoxicity against human 30M cells assessed as cell viability after 8 days by Alamar Blue assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
ISSN: 1948-5875
Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.

Research

Studies (82)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's9 (10.98)29.6817
2010's57 (69.51)24.3611
2020's16 (19.51)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.22%)5.53%
Reviews1 (1.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other80 (97.56%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
ag-490catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide
anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
2011201113.0low000010
degrasyn2011201113.0low000010
bp-1-1022013201311.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
adenine6-aminopurines;
purine nucleobase
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
201520159.0low000010
dimethyl sulfoxidesulfoxide;
volatile organic compound
alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger
202320231.0low000001
niacinamidepyridine alkaloid;
pyridinecarboxamide;
vitamin B3
anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
201520159.0low000010
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-onechromones;
morpholines;
organochlorine compound
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
201620168.0low000010
vorinostatdicarboxylic acid diamide;
hydroxamic acid
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
201520159.0low000020
temozolomideimidazotetrazine;
monocarboxylic acid amide;
triazene derivative
alkylating agent;
antineoplastic agent;
prodrug
2011201113.0low000010
pilocarpinepilocarpineantiglaucoma drug2014201410.0low000010
adenosine diphosphateadenosine 5'-phosphate;
purine ribonucleoside 5'-diphosphate
fundamental metabolite;
human metabolite
201720177.0low000010
egtazic aciddiether;
tertiary amino compound;
tetracarboxylic acid
chelator201920195.0low000010
pyrrolespyrrole;
secondary amine
202120213.0low000001
catechincatechinantioxidant;
plant metabolite
2014201410.0low000010
quinazolinesazaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
2011201113.0low000010
durapatite201920195.0low000010
vidarabinebeta-D-arabinoside;
purine nucleoside
antineoplastic agent;
bacterial metabolite;
nucleoside antibiotic
201720177.0low000010
plerixaforazacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound
anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
2013201311.0low000010
epigallocatechin gallateflavans;
gallate ester;
polyphenol
antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite
2014201410.0low000010
gefitinibaromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound
antineoplastic agent;
epidermal growth factor receptor antagonist
2011201113.0low000010
angiotensin iiamino acid zwitterion;
angiotensin II
human metabolite201720177.0low000010
sorafenib(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide
angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
201520159.0low000010
lithium chlorideinorganic chloride;
lithium salt
antimanic drug;
geroprotector
201720177.0low000010
oxytocinheterodetic cyclic peptide;
peptide hormone
oxytocic;
vasodilator agent
202020204.0low000010
fludarabinepurine nucleoside201720177.0low000010
tamoxifenstilbenoid;
tertiary amino compound
angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
2014201410.0low000010
stattic1-benzothiophenes;
C-nitro compound;
sulfone
antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor
201420207.0low000020
u 0126aryl sulfide;
dinitrile;
enamine;
substituted aniline
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
201620168.0low000010
cucurbitacin icucurbitacin;
tertiary alpha-hydroxy ketone
antineoplastic agent;
plant metabolite
2013201311.0low000010
dexmedetomidinemedetomidinealpha-adrenergic agonist;
analgesic;
non-narcotic analgesic;
sedative
202120213.0low000001
ag-490catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide
anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor
2007202011.2low000220
bay 11-7082nitrile;
sulfone
apoptosis inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor
201920195.0low000010
sq-23377cyclic ether;
enol;
polyunsaturated fatty acid;
very long-chain fatty acid
calcium ionophore;
metabolite
202320231.0low000001
panobinostatcinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound
angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
201520159.0low000010
abt-737aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound
anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
201520159.0low000010
losartan potassium201920195.0low000010
cytochrome c-t201520159.0low000010
cardiovascular agents2012201212.0low000010
incb-018424nitrile;
pyrazoles;
pyrrolopyrimidine
antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
201720177.0low000010
plx4032aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide
antineoplastic agent;
B-Raf inhibitor
2013201311.0low000010
piperidines2014201410.0low000010
interleukin-8201720177.0low000010
transforming growth factor beta201620168.0low000010
cyclin d12012201212.0low000010
nitrophenols201520159.0low000010
3-methyladenine201520159.0low000010
dacarbazinedacarbazine2011201113.0low000010
leptin200920209.5low000110
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Absence Seizure02014201410.0low000010
Absence Status02014201410.0low000010
Acute Disease02007200717.0low000100
Adenocarcinoma Of Kidney02010201014.0low000100
Adenoma, Prostatic0201820186.0low000010
Aggression0202020204.0low000010
Airway Remodeling02013201311.0low100010
Allodynia02014201410.0low000010
Angiogenesis, Pathologic02010201510.2low000130
Anoxemia0202120232.0low000002
Apnea, Obstructive Sleep0202320231.0low000001
Arthritis, Degenerative0202120213.0low000001
Asthma02013201311.0low100010
Asthma, Bronchial02013201311.0low100010
Astrocytoma, Grade IV02007201911.0low000140
B-Cell Chronic Lymphocytic Leukemia0201520197.0low000020
B-Cell Lymphoma02014201410.0low000010
B16 Melanoma02008201412.7low000120
Benign Neoplasms, Brain02007202010.6low0004110
Bladder Cancer0201720177.0low000010
Bone Cancer0201720196.0low000020
Bone Neoplasms0201720196.0low000020
Brain Neoplasms02007202010.6low0004110
Breast Cancer0201420159.5low000020
Breast Neoplasms0201420159.5low000020
Cancer of Cervix0201920195.0low000010
Cancer of Esophagus0201720177.0low000010
Cancer of Head02009201512.0low000110
Cancer of Kidney02010201014.0low000100
Cancer of Liver0202120213.0low000001
Cancer of Lung02011201312.0low000020
Cancer of Mouth02014201410.0low000020
Cancer of Nose0201620168.0low000010
Cancer of Ovary0201520178.0low000030
Cancer of Prostate0201920195.0low000010
Cancer of Skin0201320226.5low000011
Cancer of Stomach0201420216.5low000011
Cancer of the Tongue02013201410.5low000020
Carcinoma, Epidermoid02009201710.3low000160
Carcinoma, Hepatocellular0202120213.0low000001
Carcinoma, Non-Small Cell Lung02011201312.0low000020
Carcinoma, Non-Small-Cell Lung02011201312.0low000020
Carcinoma, Renal Cell02010201014.0low000100
Carcinoma, Squamous Cell02009201710.3low000160
Cardiovascular Stroke02009200915.0low000100
Chronic Disease02009201412.5low000110
Chronic Illness02009201412.5low000110
Cirrhosis0201620234.5low000011
Cognitive Decline0202320231.0low000001
Cognitive Dysfunction0202320231.0low000001
Colitis, Granulomatous0202020204.0low000010
Constriction, Pathologic02014201410.0low000010
Constriction, Pathological02014201410.0low000010
Crohn Disease0202020204.0low000010
Di Guglielmo Disease02008200816.0low000100
Diabetic Retinopathy0201920195.0low000010
Diffuse Lymphocytic Lymphoma, Poorly-Differentiated0201520159.0low000010
Disease Exacerbation0201320179.3low000030
Disease Models, Animal0200920209.0low000290
Endometrioma0201520159.0low000010
Endometriosis0201520159.0low000010
ER-Negative PR-Negative HER2-Negative Breast Cancer0201820186.0low000010
Erythremia02008200816.0low000100
Esophageal Neoplasms0201720177.0low000010
Esophageal Squamous Cell Carcinoma0201720177.0low000010
Experimental Neoplasms0201420207.0low000020
Experimental Radiation Injuries0201620168.0low000010
Fibrosis0201620234.5low000011
Fibrosis, Radiation0201620168.0low000010
Germinoblastoma0201720177.0low000010
Glial Cell Tumors02007202010.1low000250
Glioblastoma02007201911.0low000140
Glioma02007202010.1low000250
Glioma, Subependymal02014201410.0low000010
Granulocytic Leukemia02007200717.0low000100
Head and Neck Neoplasms02009201512.0low000110
Hepatocellular Carcinoma0202120213.0low000001
Hypertrophy0201720177.0low000010
Hypoxia0202120232.0low000002
Infantile Respiratory Distress Syndrome0201920195.0low000010
Inflammation0200920219.0low000101
Innate Inflammatory Response0200920219.0low000101
Invasiveness, Neoplasm0201520177.7low000030
Kahler Disease02011201113.0low000010
Kaposi Sarcoma0201520159.0low000010
Kidney Neoplasms02010201014.0low000100
Leukemia, Erythroblastic, Acute02008200816.0low000100
Leukemia, Lymphocytic, Chronic, B-Cell0201520197.0low000020
Leukemia, Myeloid02007200717.0low000100
Liver Neoplasms0202120213.0low000001
Lung Neoplasms02011201312.0low000020
Lymph Node Metastasis0201520159.0low000010
Lymphoma0201720177.0low000010
Lymphoma, B-Cell02014201410.0low000010
Lymphoma, Mantle-Cell0201520159.0low000010
Lymphoma, T-Cell0201620168.0low000010
Malignant Melanoma02009201711.0low000120
Melanoma02009201711.0low000120
Metastase0201520159.0low000010
Mouth Neoplasms02014201410.0low000020
Multiple Myeloma02011201113.0low000010
Multiple Neurofibromas0202220222.0low000001
Myocardial Infarction02009200915.0low000100
Neointima02012201212.0low000010
Neoplasm Metastasis0201520159.0low000010
Nerve Pain0201420207.0low000020
Neuralgia0201420207.0low000020
Neurilemmoma0202220222.0low000001
Neurilemoma0202220222.0low000001
Neurofibromatoses0202220222.0low000001
Obesity0201620168.0low000010
Osteoarthritis0202120213.0low000001
Osteogenic Sarcoma0201720177.0low000010
Osteosarcoma0201720177.0low000010
Ovarian Neoplasms0201520178.0low000030
Peritoneal Carcinomatosis0202120213.0low000001
Peritoneal Neoplasms0202120213.0low000001
Polycythemia Vera02008200816.0low000100
Prostatic Hyperplasia0201820186.0low000010
Prostatic Neoplasms0201920195.0low000010
Radiation Pneumonitis0201620168.0low000010
Respiratory Distress Syndrome, Newborn0201920195.0low000010
Sarcoma, Kaposi0201520159.0low000010
Scleroderma, Systemic0202320231.0low000001
Sclerosis, Systemic0202320231.0low000001
Seizures02014201410.0low000010
Skin Neoplasms0201320226.5low000011
Sleep Apnea, Obstructive0202320231.0low000001
Status Epilepticus02014201410.0low000010
Stomach Neoplasms0201420216.5low000011
T-Cell Lymphoma0201620168.0low000010
Tongue Neoplasms02013201410.5low000020
Triple Negative Breast Neoplasms0201820186.0low000010
Urinary Bladder Neoplasms0201720177.0low000010
Uterine Cervical Neoplasms0201920195.0low000010

Safety/Toxicity (1)

ArticleYear
A novel phosphorylated STAT3 inhibitor enhances T cell cytotoxicity against melanoma through inhibition of regulatory T cells.
Cancer immunology, immunotherapy : CII, , Volume: 58, Issue:7
2009

Dosage (1)

ArticleYear
The tumor microenvironment expression of p-STAT3 influences the efficacy of cyclophosphamide with WP1066 in murine melanoma models.
International journal of cancer, , Jul-01, Volume: 131, Issue:1
2012