General Information of Drug (ID: DMUGHWR)

Drug Name
WP-1066 Drug Info
Synonyms
WP1066; 857064-38-1; (S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(1-phenylethyl)acrylamide; WP 1066; UNII-63V8AIE65T; 63V8AIE65T; WP-1066; AK-99218; C17H14BrN3O; (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide; MLS006010178; SCHEMBL1315826; QCR-16; SCHEMBL1315831; GTPL7972; CHEMBL1923234; EX-A760; AOB1497; DTXSID50235007; MolPort-044-723-708; MolPort-023-219-149; ZINC13983221; AKOS016007983; WP1066/WP-1066; CS-2736; DB12679; 2-Propenamide, 3-(6-bromo-2-pyridinyl)-2-cyano-N-((1S)-1-phenylethyl)-, (2E)-; HY-15312
Indication
Disease Entry ICD 11 Status REF
Recurrent glioblastoma 2A00.00 Phase 1/2 [1]
Brain cancer 2A00 Phase 1 [2]
Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
Cross-matching ID
PubChem CID
11210478
ChEBI ID
CHEMBL1923234
CAS Number
CAS 857064-38-1
TTD Drug ID
DMUGHWR

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Preclinical Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acitretin DM8BKU9 Psoriasis vulgaris EA90 Approved [7]
Napabucasin DMDZ6Q3 Colorectal cancer 2B91.Z Phase 3 [1]
Golotimod DMKZN3A Immune System disease 4A01-4B41 Phase 2 [8]
NT219 DMOYS1N Solid tumour/cancer 2A00-2F9Z Phase 1/2 [9]
Atiprimod DM84YEC Multiple myeloma 2A83 Phase 1/2 [10]
OPB-31121 DM6VGO3 Hepatocellular carcinoma 2C12.02 Phase 1/2 [11]
IMX-110 DMNHZS4 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [1]
GLG-801 DMY1CP9 Chronic lymphocytic leukaemia 2A82.0 Phase 1/2 [1]
OPB-51602 DM760FA Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
TAK-114 DMTXE19 Ulcerative colitis DD71 Phase 1 [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
CKD-712 DMJX6SM Solid tumour/cancer 2A00-2F9Z Phase 1 [14]
Aminotriazolopyridine derivative 1 DMW2LZ0 N. A. N. A. Patented [15]
Imidazo[4,5-c]pyridine derivative 2 DMFDRJT N. A. N. A. Patented [15]
PMID27774824-Compound-Figure11Example1up DMH1W8F N. A. N. A. Patented [15]
Imidazo[4,5-c]pyridine derivative 1 DM4KBZQ N. A. N. A. Patented [15]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Momelotinib DMF98Q0 Myelofibrosis 2A20.2 Approved [16]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [17]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [18]
Quercetin DM3NC4M Obesity 5B81 Approved [19]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [20]
Paroxetine DM5PVQE Anxiety disorder 6B00-6B0Z Approved [21]
Estrone DM5T6US Acne vulgaris ED80 Approved [17]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [22]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [23]
Amlodipine DMBDAZV Angina pectoris BA40 Approved [24]
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Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [25]
Gefitinib DM15F0X Colon adenocarcinoma Approved [26]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [27]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [28]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [29]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [30]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [29]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [31]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [32]
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [36]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [37]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [38]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [39]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [40]
Gefitinib DM15F0X Colon adenocarcinoma Approved [41]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [42]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [43]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [44]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [45]
Sibutramine DMFJTDI Obesity 5B81 Approved [46]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [47]
Ardeparin DMYRX8B Deep vein thrombosis BD71 Approved [48]
Bortezomib DMNO38U Leukemia Approved [49]
Resveratrol DM3RWXL Giant cell arteritis 4A44.2 Phase 3 [6]
Tocopherol DMBIJZ6 N. A. N. A. Phase 2 [50]
MG-132 DMKA2YS N. A. N. A. Preclinical [51]
bisphenol A DM2ZLD7 Discovery agent N.A. Investigative [52]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [53]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [54]
Paclitaxel DMLB81S Breast carcinoma Approved [55]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [56]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [34]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [57]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [58]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [37]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [38]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [59]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [60]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [61]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [62]
Quizartinib DM8Y4JS Acute myeloid leukaemia 2A60 Approved [63]
Tofacitinib DMBS370 Rheumatoid arthritis FA20 Approved [64]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [65]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [66]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [67]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [68]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
JAK-STAT signaling pathway (JAK-STAT pathway) TTKAWRQ NOUNIPROTAC Inhibitor [3]
Signal transducer and activator of transcription 3 (STAT3) TTH8FZW STAT3_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [4]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [4]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [5]
Proteasome subunit beta type-5 (PSMB5) OTOZXAS6 PSB5_HUMAN Gene/Protein Processing [6]
Signal transducer and activator of transcription 5B (STAT5B) OTZVPEBT STA5B_HUMAN Post-Translational Modifications [5]
Tyrosine-protein kinase JAK2 (JAK2) OTBIDOOR JAK2_HUMAN Post-Translational Modifications [5]

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7972).
4 WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res. 2008 Feb 1;14(3):788-96. doi: 10.1158/1078-0432.CCR-07-0524.
5 WP1066 disrupts Janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res. 2007 Dec 1;67(23):11291-9. doi: 10.1158/0008-5472.CAN-07-0593.
6 Regulation of PSMB5 protein and subunits of mammalian proteasome by constitutively activated signal transducer and activator of transcription 3 (STAT3): potential role in bortezomib-mediated anticancer therapy. J Biol Chem. 2014 May 2;289(18):12612-22. doi: 10.1074/jbc.M113.542829. Epub 2014 Mar 13.
7 Effects of acitretin on the expression of signaling pathway-related genes in epidermal squamous-cell carcinoma cells. Zhonghua Zhong Liu Za Zhi. 2006 Jan;28(1):21-4.
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11 OPB-31121, a novel small molecular inhibitor, disrupts the JAK2/STAT3 pathway and exhibits an antitumor activity in gastric cancer cells. Cancer Lett. 2013 Jul 10;335(1):145-52.
12 Phase I and biomarker study of OPB-51602, a novel signal transducer and activator of transcription (STAT) 3 inhibitor, in patients with refractory solid malignancies. Ann Oncol. 2015 May;26(5):998-1005.
13 Clinical pipeline report, company report or official report of Gastroenterology.
14 HO-1 and JAK-2/STAT-1 signals are involved in preferential inhibition of iNOS over COX-2 gene expression by newly synthesized tetrahydroisoquinoline alkaloid, CKD712, in cells activated with lipopolysacchride. Cell Signal. 2008 Oct;20(10):1839-47.
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16 The effect of quercetin nanoparticle on cervical cancer progression by inducing apoptosis, autophagy and anti-proliferation via JAK2 suppression. Biomed Pharmacother. 2016 Aug;82:595-605. doi: 10.1016/j.biopha.2016.05.029. Epub 2016 Jun 9.
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19 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
20 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
21 Paroxetine modulates immune responses by activating a JAK2/STAT3 signaling pathway. J Biochem Mol Toxicol. 2020 May;34(5):e22464. doi: 10.1002/jbt.22464. Epub 2020 Feb 5.
22 A comprehensive analysis of Wnt/beta-catenin signaling pathway-related genes and crosstalk pathways in the treatment of As2O3 in renal cancer. Ren Fail. 2018 Nov;40(1):331-339.
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24 Amlodipine inhibits cell proliferation via PKD1-related pathway. Biochem Biophys Res Commun. 2008 May 2;369(2):376-81. doi: 10.1016/j.bbrc.2008.02.075. Epub 2008 Feb 25.
25 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
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31 Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
32 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
33 Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
34 Treatment with anticancer agents induces dysregulation of specific Wnt signaling pathways in human ovarian luteinized granulosa cells in vitro. Toxicol Sci. 2013 Nov;136(1):183-92. doi: 10.1093/toxsci/kft175. Epub 2013 Aug 16.
35 Progesterone increases csk homologous kinase in HMC-1560 human mast cells and reduces cell proliferation. J Cell Biochem. 2007 Dec 1;102(5):1271-80. doi: 10.1002/jcb.21357.
36 Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
37 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
38 Growth stimulation of human pulmonary adenocarcinoma cells and small airway epithelial cells by beta-carotene via activation of cAMP, PKA, CREB and ERK1/2. Int J Cancer. 2006 Mar 15;118(6):1370-80. doi: 10.1002/ijc.21537.
39 Estrogen and pure antiestrogen fulvestrant (ICI 182 780) augment cell-matrigel adhesion of MCF-7 breast cancer cells through a novel G protein coupled estrogen receptor (GPR30)-to-calpain signaling axis. Toxicol Appl Pharmacol. 2014 Mar 1;275(2):176-81. doi: 10.1016/j.taap.2014.01.005. Epub 2014 Jan 17.
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41 Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. Breast Cancer Res Treat. 2010 Feb;119(3):575-91. doi: 10.1007/s10549-009-0355-8. Epub 2009 Mar 15.
42 Effect of histamine H1 receptor antagonists on TARC/CCL17 and MDC/CCL22 production from CD14+ cells induced by antigenic stimulation in vitro. Int Arch Allergy Immunol. 2011;155(1):38-51. doi: 10.1159/000318720. Epub 2010 Nov 25.
43 SIRT3 Mediates the Antioxidant Effect of Hydrogen Sulfide in Endothelial Cells. Antioxid Redox Signal. 2016 Feb 20;24(6):329-43. doi: 10.1089/ars.2015.6331. Epub 2015 Nov 10.
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45 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
46 Sibutramine provokes apoptosis of aortic endothelial cells through altered production of reactive oxygen and nitrogen species. Toxicol Appl Pharmacol. 2017 Jan 1;314:1-11. doi: 10.1016/j.taap.2016.11.003. Epub 2016 Nov 9.
47 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
48 Biochemical and toxicological evaluation of nano-heparins in cell functional properties, proteasome activation and expression of key matrix molecules. Toxicol Lett. 2016 Jan 5;240(1):32-42. doi: 10.1016/j.toxlet.2015.10.005. Epub 2015 Oct 22.
49 Molecular mechanisms of bortezomib resistant adenocarcinoma cells. PLoS One. 2011;6(12):e27996. doi: 10.1371/journal.pone.0027996. Epub 2011 Dec 22.
50 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
51 The role of PSMB5 in sodium arsenite-induced oxidative stress in L-02 cells. Cell Stress Chaperones. 2020 May;25(3):533-540. doi: 10.1007/s12192-020-01104-1. Epub 2020 Apr 16.
52 Alternatives for the worse: Molecular insights into adverse effects of bisphenol a and substitutes during human adipocyte differentiation. Environ Int. 2021 Nov;156:106730. doi: 10.1016/j.envint.2021.106730. Epub 2021 Jun 27.
53 Downregulation of mitogen-activated protein kinases (MAPKs) in chronic ethanol-induced fatty liver. Toxicol Mech Methods. 2020 Jul;30(6):407-416. doi: 10.1080/15376516.2020.1747126. Epub 2020 Apr 1.
54 A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling. Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. doi: 10.1073/pnas.0707936104. Epub 2007 Oct 9.
55 The stent-eluting drugs sirolimus and paclitaxel suppress healing of the endothelium by induction of autophagy. Am J Pathol. 2009 Nov;175(5):2226-34.
56 Modulation of apoptosis in HaCaT keratinocytes via differential regulation of ERK signaling pathway by flavonoids. J Biol Chem. 2005 Sep 9;280(36):31498-507. doi: 10.1074/jbc.M505537200. Epub 2005 Jul 13.
57 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
58 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
59 Oxidative stress triggers STAT3 tyrosine phosphorylation and nuclear translocation in human lymphocytes. J Biol Chem. 1999 Jun 18;274(25):17580-6. doi: 10.1074/jbc.274.25.17580.
60 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
61 Arsenic trioxide down-regulates antiapoptotic genes and induces cell death in mycosis fungoides tumors in a mouse model. Ann Oncol. 2008 Aug;19(8):1488-1494. doi: 10.1093/annonc/mdn056. Epub 2008 Mar 17.
62 Expression profile analysis of human peripheral blood mononuclear cells in response to aspirin. Arch Immunol Ther Exp (Warsz). 2005 Mar-Apr;53(2):151-8.
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64 Janus kinase 3-activating mutations identified in natural killer/T-cell lymphoma. Cancer Discov. 2012 Jul;2(7):591-7. doi: 10.1158/2159-8290.CD-12-0028. Epub 2012 Jun 15.
65 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
66 Differential effect of dexamethasone on cell death and STAT5 activation during in vitro eosinopoiesis. Br J Haematol. 2003 Dec;123(5):933-41. doi: 10.1046/j.1365-2141.2003.04700.x.
67 Drug-induced endoplasmic reticulum and oxidative stress responses independently sensitize toward TNF-mediated hepatotoxicity. Toxicol Sci. 2014 Jul;140(1):144-59. doi: 10.1093/toxsci/kfu072. Epub 2014 Apr 20.
68 Progesterone pre-treatment potentiates EGF pathway signaling in the breast cancer cell line ZR-75. Breast Cancer Res Treat. 2005 Nov;94(2):171-83. doi: 10.1007/s10549-005-7726-6.