General Information of Drug (ID: DMD3CUJ)

Drug Name
T-5224 Drug Info
Synonyms AKOS003047196; T5224
Indication
Disease Entry ICD 11 Status REF
Rheumatoid arthritis FA20 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
23626877
ChEBI ID
CHEMBL3222137
TTD Drug ID
DMD3CUJ

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Investigative Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
TWS-119 DMS29M4 Discovery agent N.A. Investigative [4]
PNRI-299 DMDBZGP Discovery agent N.A. Investigative [5]
TAM-67 DM26SE7 Discovery agent N.A. Investigative [6]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [7]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [8]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [9]
Gefitinib DM15F0X Colon adenocarcinoma Approved [10]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [11]
Selenium DM25CGV N. A. N. A. Approved [12]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [13]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [14]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
⏷ Show the Full List of 10 Drug(s)
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 [17]
Gefitinib DM15F0X Colon adenocarcinoma Approved [18]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [19]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [20]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [21]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [22]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [21]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [23]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [24]
Methotrexate DM2TEOL Anterior urethra cancer Approved [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [26]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [27]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [28]
Quercetin DM3NC4M Obesity 5B81 Approved [29]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [30]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [31]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [32]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [33]
Nilotinib DM7HXWT Chronic myelogenous leukaemia 2A20.0 Approved [34]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [35]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [36]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [37]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [38]
Bortezomib DMNO38U Leukemia Approved [3]
Arsenic DMTL2Y1 N. A. N. A. Approved [39]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [40]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [41]
phorbol 12-myristate 13-acetate DMJWD62 Acute myeloid leukaemia 2A60 Phase 2 [42]
(+)-JQ1 DM1CZSJ Testicular cancer 2C80 Phase 1 [43]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [44]
⏷ 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
Transcription factor AP-1 (JUN) TTN3GBV JUN_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Interferon regulatory factor 4 (IRF4) OT1DHQ1P IRF4_HUMAN Gene/Protein Processing [3]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Gene/Protein Processing [3]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [3]
Transcription factor JunB (JUNB) OTG2JXV5 JUNB_HUMAN Gene/Protein Processing [3]

References

1 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016746)
2 CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
3 The selective activator protein-1 inhibitor T-5224 regulates the IRF4/MYC axis and exerts cooperative antimyeloma activity with bortezomib. Chem Biol Interact. 2023 Oct 1;384:110687. doi: 10.1016/j.cbi.2023.110687. Epub 2023 Aug 31.
4 Diversity-oriented synthesis: exploring the intersections between chemistry and biology. Nat Chem Biol. 2005 Jul;1(2):74-84.
5 Chemogenomic identification of Ref-1/AP-1 as a therapeutic target for asthma. Proc Natl Acad Sci U S A. 2003 Feb 4;100(3):1169-73.
6 AP-1 blockade inhibits the growth of normal and malignant breast cells. Oncogene. 2001 May 17;20(22):2771-80.
7 Acetaminophen-induced proliferation of estrogen-responsive breast cancer cells is associated with increases in c-myc RNA expression and NF-kappaB activity. Toxicol Sci. 2002 Apr;66(2):233-43. doi: 10.1093/toxsci/66.2.233.
8 Sertraline induces endoplasmic reticulum stress in hepatic cells. Toxicology. 2014 Aug 1;322:78-88. doi: 10.1016/j.tox.2014.05.007. Epub 2014 May 24.
9 Estrogen regulation in human breast cancer cells of new downstream gene targets involved in estrogen metabolism, cell proliferation and cell transformation. J Mol Endocrinol. 2004 Apr;32(2):397-414.
10 ZD1839 induces p15INK4b and causes G1 arrest by inhibiting the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway. Mol Cancer Ther. 2007 May;6(5):1579-87. doi: 10.1158/1535-7163.MCT-06-0814.
11 Arsenic suppresses gene expression in promyelocytic leukemia cells partly through Sp1 oxidation. Blood. 2005 Jul 1;106(1):304-10.
12 Selenite and selenomethionine promote HL-60 cell cycle progression. J Nutr. 2002 Apr;132(4):674-9. doi: 10.1093/jn/132.4.674.
13 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
14 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
15 Novel detection and differential utilization of a c-myc transcriptional block in colon cancer chemoprevention. Cancer Res. 2002 Nov 1;62(21):6006-10.
16 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
17 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.
18 Evidence of securin-mediated resistance to gefitinib-induced apoptosis in human cancer cells. Chem Biol Interact. 2013 Apr 25;203(2):412-22. doi: 10.1016/j.cbi.2013.03.011. Epub 2013 Mar 22.
19 Cigarette smoke and asbestos activate poly-ADP-ribose polymerase in alveolar epithelial cells. J Investig Med. 2001 Jan;49(1):68-76. doi: 10.2310/6650.2001.34092.
20 Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
21 The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47. doi: 10.1002/(sici)1099-0461(1999)13:6<338::aid-jbt8>3.0.co;2-7.
22 Ciprofloxacin mediated cell growth inhibition, S/G2-M cell cycle arrest, and apoptosis in a human transitional cell carcinoma of the bladder cell line. Clin Cancer Res. 2000 Mar;6(3):891-900.
23 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.
24 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
25 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.
26 Nitrogen mustard prevents transport of Fra-1 into the nucleus to promote c-Fos- and FosB-dependent IL-8 induction in injured mouse epidermis. Toxicol Lett. 2020 Feb 1;319:256-263. doi: 10.1016/j.toxlet.2019.10.006. Epub 2019 Oct 19.
27 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
28 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
29 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.
30 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
31 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.
32 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
33 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
34 Endoplasmic reticulum stress-mediated apoptosis in imatinib-resistant leukemic K562-r cells triggered by AMN107 combined with arsenic trioxide. Exp Biol Med (Maywood). 2013 Aug 1;238(8):932-42. doi: 10.1177/1535370213492689. Epub 2013 Jul 24.
35 DNA microarray analysis of vitamin D-induced gene expression in a human colon carcinoma cell line. Physiol Genomics. 2004 Apr 13;17(2):122-9. doi: 10.1152/physiolgenomics.00002.2003.
36 Simvastatin inhibits IFN regulatory factor 4 expression and Th17 cell differentiation in CD4+ T cells derived from patients with multiple sclerosis. J Immunol. 2011 Sep 15;187(6):3431-7. doi: 10.4049/jimmunol.1100580. Epub 2011 Aug 19.
37 Analysis of the transcriptional regulation of cancer-related genes by aberrant DNA methylation of the cis-regulation sites in the promoter region during hepatocyte carcinogenesis caused by arsenic. Oncotarget. 2015 Aug 28;6(25):21493-506. doi: 10.18632/oncotarget.4085.
38 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
39 Transcriptomics and methylomics of CD4-positive T cells in arsenic-exposed women. Arch Toxicol. 2017 May;91(5):2067-2078. doi: 10.1007/s00204-016-1879-4. Epub 2016 Nov 12.
40 Predictive toxicology using systemic biology and liver microfluidic "on chip" approaches: application to acetaminophen injury. Toxicol Appl Pharmacol. 2012 Mar 15;259(3):270-80.
41 ON 01910.Na is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Clin Cancer Res. 2012 Apr 1;18(7):1979-91. doi: 10.1158/1078-0432.CCR-11-2113. Epub 2012 Feb 20.
42 The effects of Phorbol 12-myristate 13-acetate concentration on the expression of miR-155 and miR-125b and their macrophage function-related genes in the U937 cell line. J Toxicol Sci. 2020;45(12):751-761. doi: 10.2131/jts.45.751.
43 Selective inhibition of tumor oncogenes by disruption of super-enhancers. Cell. 2013 Apr 11;153(2):320-34. doi: 10.1016/j.cell.2013.03.036.
44 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.