General Information of Drug (ID: DM7XZY5)

Drug Name
Triapine Drug Info
Synonyms
Triapine; 236392-56-6; 143621-35-6; 3-Apct; Pan 811; 3-Aminopyridine-2-carboxaldehyde thiosemicarbazone; 3-AP; UNII-U4XIL4091C; NSC 663249; 200933-27-3; OCX 191; 2-((3-Aminopyridin-2-yl)methylene)hydrazinecarbothioamide; C7H9N5S; PAN-811; U4XIL4091C; 3-aminopyridine-2-carbaldehyde-thiosemicarbazone; [(E)-(3-amino-2-pyridyl)methyleneamino]thiourea; 3-Aminopyridine-2-carboxaldehyde- thiosemicarbazone; Hydrazinecarbothioamide, 2-((3-amino-2-pyridinyl)methylene)-; (E)-2-((3-aminopyridin-2-yl)methylene)hydrazinecarbothioamide
Indication
Disease Entry ICD 11 Status REF
Nerve injury ND56.4 Phase 2 [1]
Cross-matching ID
PubChem CID
9571836
CAS Number
CAS 143621-35-6
TTD Drug ID
DM7XZY5

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Preclinical Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [4]
Hydroxyurea DMOQVU9 Chronic myelogenous leukaemia 2A20.0 Approved [4]
CO-101 DMH5GQU Pancreatic cancer 2C10 Phase 2 [5]
CALAA-01 DMT4Z5B Solid tumour/cancer 2A00-2F9Z Phase 1 [6]
LY-2334737 DMCBV20 Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
Gallium maltolate DMX0Z51 Human immunodeficiency virus infection 1C62 Discontinued in Phase 2 [8]
MDL 101,731 DMKEYSX Gastric adenocarcinoma 2B72 Discontinued in Phase 2 [9]
NKP-46 DMK8UD0 Solid tumour/cancer 2A00-2F9Z Preclinical [10]
⏷ Show the Full List of 8 Drug(s)
Drug(s) Affected By Histone H2AX (H2AX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [12]
Selenium DM25CGV N. A. N. A. Approved [13]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [14]
Etretinate DM2CZFA Keratosis ED56 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [17]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [18]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [19]
Quercetin DM3NC4M Obesity 5B81 Approved [20]
⏷ 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 [21]
Quercetin DM3NC4M Obesity 5B81 Approved [22]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [23]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [24]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [25]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [26]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [27]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [28]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [29]
Aminoglutethimide DMWFHMZ Cushing disease 5A70 Approved [30]
⏷ 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
Ribonucleoside-diphosphate reductase M2 (RRM2) TTBWDI0 RIR2_HUMAN Modulator [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Histone H2AX (H2AX) OT18UX57 H2AX_HUMAN Gene/Protein Processing [2]
Thioredoxin, mitochondrial OTE9A5XQ THIOM_HUMAN Post-Translational Modifications [3]
Thioredoxin-dependent peroxide reductase, mitochondrial (PRDX3) OTLB2WEU PRDX3_HUMAN Post-Translational Modifications [3]

References

1 PAN-811 inhibits oxidative stress-induced cell death of human Alzheimer's disease-derived and age-matched olfactory neuroepithelial cells via suppression of intracellular reactive oxygen species. J Alzheimers Dis. 2009;17(3):611-9.
2 Distinct mechanisms of cell-kill by triapine and its terminally dimethylated derivative Dp44mT due to a loss or gain of activity of their copper(II) complexes. Biochem Pharmacol. 2014 Oct 1;91(3):312-22. doi: 10.1016/j.bcp.2014.08.006. Epub 2014 Aug 15.
3 The iron-chelating drug triapine causes pronounced mitochondrial thiol redox stress. Toxicol Lett. 2011 Mar 5;201(2):130-6. doi: 10.1016/j.toxlet.2010.12.017. Epub 2010 Dec 31.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 Cellular pharmacology of gemcitabine. Ann Oncol. 2006 May;17 Suppl 5:v7-12.
6 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
7 Phase I study of oral gemcitabine prodrug (LY2334737) in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2013 Jun;71(6):1645-55.
8 Gallium maltolate is a promising chemotherapeutic agent for the treatment of hepatocellular carcinoma. Anticancer Res. 2006 May-Jun;26(3A):1739-43.
9 Tezacitabine Hoechst Marion Roussel.Curr Opin Investig Drugs.2000 Sep;1(1):135-40.
10 Phase I and pharmacokinetic study of the oral tris-(8-quinolinolato)gallium(III) complex (FFC11, KP46) in patients with solid tumors - a study of the CESAR Central European Society for Anticancer Drug Research - EWIV. J Clin Oncol (Meeting Abstracts) June 2005 vol. 23 no. 16_suppl 3205.
11 Cannabinoids synergize with carfilzomib, reducing multiple myeloma cells viability and migration. Oncotarget. 2016 Nov 22;7(47):77543-77557. doi: 10.18632/oncotarget.12721.
12 Hsa-let-7g miRNA regulates the anti-tumor effects of gastric cancer cells under oxidative stress through the expression of DDR genes. J Toxicol Sci. 2015 Jun;40(3):329-38. doi: 10.2131/jts.40.329.
13 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.
14 Inhibition of cardiomyocyte differentiation of human induced pluripotent stem cells by Ribavirin: Implication for its cardiac developmental toxicity. Toxicology. 2020 Apr 15;435:152422. doi: 10.1016/j.tox.2020.152422. Epub 2020 Feb 26.
15 Synthesis and structure-activity relationships of new antiproliferative and proapoptotic retinoid-related biphenyl-4-yl-acrylic acids. Bioorg Med Chem. 2007 Jul 15;15(14):4863-75. doi: 10.1016/j.bmc.2007.04.057. Epub 2007 May 3.
16 Methotrexate induces apoptosis through p53/p21-dependent pathway and increases E-cadherin expression through downregulation of HDAC/EZH2. Biochem Pharmacol. 2011 Feb 15;81(4):510-7. doi: 10.1016/j.bcp.2010.11.014. Epub 2010 Nov 27.
17 Actinomycin D inhibits the expression of the cystine/glutamate transporter xCT via attenuation of CD133 synthesis in CD133(+) HCC. Chem Biol Interact. 2019 Aug 25;309:108713. doi: 10.1016/j.cbi.2019.06.026. Epub 2019 Jun 19.
18 Simvastatin and purine analogs have a synergic effect on apoptosis of chronic lymphocytic leukemia cells. Ann Hematol. 2010 Nov;89(11):1115-24. doi: 10.1007/s00277-010-0988-z. Epub 2010 May 25.
19 The involvement of hepatic cytochrome P450s in the cytotoxicity of lapatinib. Toxicol Sci. 2023 Dec 21;197(1):69-78. doi: 10.1093/toxsci/kfad099.
20 The isoflavonoids genistein and quercetin activate different stress signaling pathways as shown by analysis of site-specific phosphorylation of ATM, p53 and histone H2AX. DNA Repair (Amst). 2004 Mar 4;3(3):235-44. doi: 10.1016/j.dnarep.2003.10.014.
21 MS4A3-HSP27 target pathway reveals potential for haematopoietic disorder treatment in alimentary toxic aleukia. Cell Biol Toxicol. 2023 Feb;39(1):201-216. doi: 10.1007/s10565-021-09639-4. Epub 2021 Sep 28.
22 Quercetin induces the expression of peroxiredoxins 3 and 5 via the Nrf2/NRF1 transcription pathway. Invest Ophthalmol Vis Sci. 2011 Feb 22;52(2):1055-63. doi: 10.1167/iovs.10-5777.
23 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.
24 Downregulation of the c-MYC target gene, peroxiredoxin III, contributes to arsenic trioxide-induced apoptosis in acute promyelocytic leukemia. Int J Cancer. 2009 Jul 15;125(2):264-75. doi: 10.1002/ijc.24341.
25 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
26 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.
27 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
28 Mitochondrial proteomics investigation of a cellular model of impaired dopamine homeostasis, an early step in Parkinson's disease pathogenesis. Mol Biosyst. 2014 Jun;10(6):1332-44.
29 Multiple microRNAs function as self-protective modules in acetaminophen-induced hepatotoxicity in humans. Arch Toxicol. 2018 Feb;92(2):845-858.
30 Proteomic profile of aminoglutethimide-induced apoptosis in HL-60 cells: role of myeloperoxidase and arylamine free radicals. Chem Biol Interact. 2015 Sep 5;239:129-38.