General Information of Drug (ID: DMG5OZP)

Drug Name
Fascaplysin Drug Info
Synonyms
Pyrido[1,2-a:3,4-b']diindol-5-ium,12,13-dihydro-13-oxo-, chloride; GNF-PF-1458; ACMC-20bu3v; AC1L2JLY; AC1Q6JA3; SCHEMBL1728912; CHEMBL602937; GTPL5969; BDBM59087; CTK4A8872; CHEBI:93765; ZINC1616841; pyrido[1,2-a:3,4-b']diindol-5-ium, 12,13-dihydro-13-oxo-; HSCI1_000331; NCGC00346951-01; CJ-26101; BRD-K13287209-003-03-2; BRD-K13287209-311-02-1; BRD-K13287209-311-01-3; BRD-K13287209-003-02-4; BRD-K13287209-003-01-6
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
73292
ChEBI ID
CHEMBL258765
CAS Number
CAS 114719-57-2
TTD Drug ID
DMG5OZP

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [4]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [5]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [6]
Ribociclib Succinate DM9CIUW Breast cancer 2C60-2C65 Approved [7]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [8]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [9]
Ro 31-7453 DM83QCL Solid tumour/cancer 2A00-2F9Z Phase 2 [10]
P276-00 DM9DJL2 Mantle cell lymphoma 2A85.5 Phase 2 [11]
P-276 DMMJUHD Breast cancer 2C60-2C65 Phase 2 [12]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apremilast DMTWS9E Psoriasis vulgaris EA90 Approved [4]
LY2835219 DM93VBZ Breast cancer 2C60-2C65 Approved [5]
Palbociclib DMD7L94 Breast cancer 2C60-2C65 Approved [6]
Ribociclib Succinate DM9CIUW Breast cancer 2C60-2C65 Approved [7]
Trilaciclib DMP5A4T Small-cell lung cancer 2C25.Y Approved [8]
LEE011 DMMX75K Breast cancer 2C60-2C65 Phase 3 [9]
G1T38 DMQO2IT Breast cancer 2C60-2C65 Phase 2 [13]
GLR2007 DM7DWLY Glioblastoma of brain 2A00.00 Phase 1/2 [14]
FCN-437 DMQ8VUW Breast cancer 2C60-2C65 Phase 1/2 [15]
NUV-422 DMQJQNT Malignant glioma 2A00.0 Phase 1/2 [16]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [17]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [18]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [19]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [20]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [21]
Ibuprofen DM8VCBE Dysmenorrhea GA34.3 Approved [22]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [23]
Momelotinib DMF98Q0 Myelofibrosis 2A20.2 Approved [24]
Flurbiprofen DMGN4BY Osteoarthritis FA00-FA05 Approved [22]
Cupric Sulfate DMP0NFQ Fungal infection 1F29-1F2F Approved [25]
⏷ 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 [26]
Gefitinib DM15F0X Colon adenocarcinoma Approved [27]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [28]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [29]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [30]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [31]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [30]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [32]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [33]
Methotrexate DM2TEOL Anterior urethra cancer Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [35]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [36]
Quercetin DM3NC4M Obesity 5B81 Approved [37]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [38]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [39]
Adenosine triphosphate DM79F6G Malnutrition 5B50-5B71 Approved [40]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [41]
Cantharidin DMBP5N3 Molluscum contagiosum infection 1E76 Approved [42]
Atorvastatin DMF28YC Acute coronary syndrome BA41 Approved [43]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [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
Cyclin-dependent kinase 4 (CDK4) TT0PG8F CDK4_HUMAN Inhibitor [2]
Cyclin-dependent kinase 6 (CDK6) TTO0FDJ CDK6_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Eukaryotic translation initiation factor 4E (EIF4E) OTDAWNLA IF4E_HUMAN Post-Translational Modifications [3]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) OTTOMI8J PK3CA_HUMAN Gene/Protein Processing [3]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [3]

References

1 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: 5969).
2 Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25.
3 A marine sponge alkaloid derivative 4-chloro fascaplysin inhibits tumor growth and VEGF mediated angiogenesis by disrupting PI3K/Akt/mTOR signaling cascade. Chem Biol Interact. 2017 Sep 25;275:47-60.
4 Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc. 2005.
5 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2017
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
9 Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82.
10 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
11 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
12 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154.
13 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
14 Clinical pipeline report, company report or official report of Gan & Lee Pharmaceuticals.
15 Clinical pipeline report, company report or official report of Fochon Pharmaceuticals.
16 ClinicalTrials.gov (NCT04541225) Phase 1/2 Dose Escalation, Safety, Pharmacokinetics, and Efficacy Study of NUV-422 in Adults With Recurrent or Refractory High-grade Gliomas and Solid Tumors. U.S.National Institutes of Health.
17 Ribavirin inhibits the growth and ascites formation of hepatocellular carcinoma through downregulation of type I CARM1 and type II PRMT5. Toxicol Appl Pharmacol. 2022 Jan 15;435:115829. doi: 10.1016/j.taap.2021.115829. Epub 2021 Dec 14.
18 Benzodithiophenes potentiate differentiation of acute promyelocytic leukemia cells by lowering the threshold for ligand-mediated corepressor/coactivator exchange with retinoic acid receptor alpha and enhancing changes in all-trans-retinoic acid-regulated gene expression. Cancer Res. 2005 Sep 1;65(17):7856-65. doi: 10.1158/0008-5472.CAN-05-1056.
19 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
20 Differential Response of Glioma Stem Cells to Arsenic Trioxide Therapy Is Regulated by MNK1 and mRNA Translation. Mol Cancer Res. 2018 Jan;16(1):32-46. doi: 10.1158/1541-7786.MCR-17-0397. Epub 2017 Oct 17.
21 A systems biology understanding of the synergistic effects of arsenic sulfide and Imatinib in BCR/ABL-associated leukemia. Proc Natl Acad Sci U S A. 2009 Mar 3;106(9):3378-83.
22 The p38 MAPK pathway mediates aryl propionic acid induced messenger rna stability of p75 NTR in prostate cancer cells. Cancer Res. 2007 Dec 1;67(23):11402-10. doi: 10.1158/0008-5472.CAN-07-1792.
23 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.
24 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.
25 Physiological and toxicological transcriptome changes in HepG2 cells exposed to copper. Physiol Genomics. 2009 Aug 7;38(3):386-401.
26 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.
27 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.
28 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.
29 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.
30 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.
31 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.
32 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.
33 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
34 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.
35 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.
36 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.
37 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.
38 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.
39 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.
40 The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d.
41 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
42 Cantharidin suppresses gastric cancer cell migration/invasion by inhibiting the PI3K/Akt signaling pathway via CCAT1. Chem Biol Interact. 2020 Feb 1;317:108939. doi: 10.1016/j.cbi.2020.108939. Epub 2020 Jan 13.
43 Atorvastatin induces MicroRNA-145 expression in HEPG2 cells via regulation of the PI3K/AKT signalling pathway. Chem Biol Interact. 2018 May 1;287:32-40. doi: 10.1016/j.cbi.2018.04.005. Epub 2018 Apr 6.
44 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.