General Information of Drug (ID: DM4T5DY)

Drug Name
FGIN-1-27 Drug Info
Synonyms
FGIN-1-27; 142720-24-9; N,N-Dihexyl-2-(4-fluorophenyl)indole-3-acetamide; Fgin 1 27; Fgin 1-27; N,N-Di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide; CHEMBL63154; 1H-Indole-3-acetamide, 2-(4-fluorophenyl)-N,N-dihexyl-; 2-(2-(4-fluorophenyl)-1H-indol-3-yl)-N,N-dihexylacetamide; 2-[2-(4-fluorophenyl)-1H-indol-3-yl]-N,N-dihexylacetamide; SR-01000075838; Tocris-0658; Lopac-D-8555; Biomol-NT_000279; Lopac0_000453; MLS002153299; SCHEMBL1229718; BPBio1_001277; AC1L313J; FGIN1-27; CHEBI:92171; CTK8E7869; DTXSID90162141
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
132496
ChEBI ID
CHEBI:92171
CAS Number
CAS 142720-24-9
TTD Drug ID
DM4T5DY

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Translocator protein (TSPO)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Diazepam DM08E9O Alcohol withdrawal Approved [4]
Flunitrazepam DMGR5Z3 Insomnia 7A00-7A0Z Approved [5]
Oxazepam DMXNZM4 Alcohol withdrawal delirium Approved [6]
Midazolam DMXOELT Agitation 6A70.3 Approved [7]
Temazepam DM02A65 Insomnia 7A00-7A0Z Approved [7]
Flumazenil DMPCG2L Benzodiazepine overdose PC91 Approved [8]
Alprazolam DMC7XDN Anxiety Approved [5]
Clotiazepam DM59AZT Anxiety disorder 6B00-6B0Z Approved [9]
Quazepam DMY4D87 Insomnia 7A00-7A0Z Approved [7]
Eszopiclone DM8RZ9H Insomnia 7A00-7A0Z Approved [10]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [11]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [12]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [13]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [14]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [15]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [15]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [16]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [17]
Capsaicin DMGMF6V Back pain ME84.Z Approved [18]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2B6 (CYP2B6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [20]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [21]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [22]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [23]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [24]
Clopidogrel DMOL54H Acute coronary syndrome BA41 Approved [25]
Artemisinin DMOY7W3 Malaria 1F40-1F45 Approved [26]
Malathion DMXZ84M Pediculus capitis infestation 1G00.0 Approved [27]
Phenobarbital DMXZOCG Cluster headache 8A81.0 Approved [28]
Permethrin DMZ0Q1G Pediculus capitis infestation 1G00.0 Approved [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [30]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [31]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [32]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [33]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [34]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [35]
Verapamil DMA7PEW Angina pectoris BA40 Approved [36]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [37]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [38]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [39]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-3 (CASP3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [40]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [41]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [42]
Cidofovir DMA13GD Cytomegalovirus infection 1D82 Approved [43]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [44]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [45]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [46]
Mannitol DMSCDY9 Bronchiectasis CA24 Approved [47]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [48]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [49]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Apoptosis regulator BAX (BAX)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [30]
Aprepitant DM053KT Depression 6A70-6A7Z Approved [49]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [35]
Verapamil DMA7PEW Angina pectoris BA40 Approved [36]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [50]
Leuprorelin acetate DM15HAT Prostate cancer 2C82.0 Approved [51]
Talazoparib DM1KS78 Breast cancer 2C60-2C65 Approved [52]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [53]
Meloxicam DM2AR7L Arthritis FA20 Approved [54]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [55]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Bcl-2-like protein 1 (BCL2L1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [56]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [57]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [58]
Selenium DM25CGV N. A. N. A. Approved [59]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [60]
Methotrexate DM2TEOL Anterior urethra cancer Approved [61]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [62]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [63]
Quercetin DM3NC4M Obesity 5B81 Approved [64]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [65]
⏷ 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
Translocator protein (TSPO) TTPTXIN TSPO_HUMAN Binder [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Gene/Protein Processing [2]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [2]
Bcl-2-like protein 1 (BCL2L1) OTRC5K9O B2CL1_HUMAN Gene/Protein Processing [2]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Gene/Protein Processing [2]
Cytochrome P450 2B6 (CYP2B6) OTOYO4S7 CP2B6_HUMAN Gene/Protein Processing [3]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Gene/Protein Processing [3]

References

1 Specific ligands of the peripheral benzodiazepine receptor induce apoptosis and cell cycle arrest in human colorectal cancer cells. Br J Cancer. 2001 Nov 30;85(11):1771-80.
2 Peripheral benzodiazepine receptor ligands induce apoptosis and cell cycle arrest in human hepatocellular carcinoma cells and enhance chemosensitivity to paclitaxel, docetaxel, doxorubicin and the Bcl-2 inhibitor HA14-1. J Hepatol. 2004 Nov;41(5):799-807. doi: 10.1016/j.jhep.2004.07.015.
3 Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR). Toxicol Lett. 2011 Apr 25;202(2):148-54.
4 Translocator protein (18 kDa) mediates the pro-growth effects of diazepam on Ehrlich tumor cells in vivo. Eur J Pharmacol. 2010 Jan 25;626(2-3):131-8.
5 Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation. J Pharmacol Sci. 2009 May;110(1):36-46.
6 Effects of the combination of metyrapone and oxazepam on cocaine and food self-administration in rats. Pharmacol Biochem Behav. 2008 Nov;91(1):181-9.
7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
8 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. (Target id: 2879).
9 Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones. Br J Pharmacol. 1989 Nov;98(3):735-40.
10 New hypnotics: perspectives from sleep physiology. Vertex. 2007 Jul-Aug;18(74):294-9.
11 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
12 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
13 Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
14 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
15 Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
16 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
17 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
18 Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
19 Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
20 Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class. Toxicol Lett. 2016 Jan 22;241:82-94.
21 Transcriptional profiling suggests that Nevirapine and Ritonavir cause drug induced liver injury through distinct mechanisms in primary human hepatocytes. Chem Biol Interact. 2016 Aug 5;255:31-44.
22 Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.
23 Thalidomide increases human hepatic cytochrome P450 3A enzymes by direct activation of the pregnane X receptor. Chem Res Toxicol. 2014 Feb 17;27(2):304-308.
24 Human constitutive androstane receptor mediates induction of CYP2B6 gene expression by phenytoin. J Biol Chem. 2004 Jul 9;279(28):29295-301. doi: 10.1074/jbc.M400580200. Epub 2004 Apr 28.
25 Identification of novel agonists by high-throughput screening and molecular modelling of human constitutive androstane receptor isoform 3. Arch Toxicol. 2019 Aug;93(8):2247-2264. doi: 10.1007/s00204-019-02495-6. Epub 2019 Jul 16.
26 Antimalarial artemisinin drugs induce cytochrome P450 and MDR1 expression by activation of xenosensors pregnane X receptor and constitutive androstane receptor. Mol Pharmacol. 2005 Jun;67(6):1954-65.
27 Characterization of human cytochrome P450 induction by pesticides. Toxicology. 2012 Mar 29;294(1):17-26.
28 Species-specific mechanisms for cholesterol 7alpha-hydroxylase (CYP7A1) regulation by drugs and bile acids. Arch Biochem Biophys. 2005 Feb 1;434(1):75-85.
29 Pyrethroids: cytotoxicity and induction of CYP isoforms in human hepatocytes. Drug Metabol Drug Interact. 2008;23(3-4):211-36.
30 4.8% sevoflurane induces activation of autophagy in human neuroblastoma SH-SY5Y cells by the AMPK/mTOR signaling pathway. Neurotoxicology. 2022 May;90:256-264. doi: 10.1016/j.neuro.2022.04.008. Epub 2022 Apr 23.
31 Enhanced chemotherapeutic efficacy of docetaxel in human lung cancer cell line via GLUT1 inhibitor. J Biochem Mol Toxicol. 2023 Jun;37(6):e23348. doi: 10.1002/jbt.23348. Epub 2023 Mar 31.
32 Breast cancer cells response to the antineoplastic agents cisplatin, carboplatin, and doxorubicin at the mRNA expression levels of distinct apoptosis-related genes, including the new member, BCL2L12. Ann N Y Acad Sci. 2007 Jan;1095:35-44. doi: 10.1196/annals.1397.005.
33 Extracellular signal-regulated kinase activation and Bcl-2 downregulation mediate apoptosis after gemcitabine treatment partly via a p53-independent pathway. Eur J Pharmacol. 2004 Oct 19;502(3):169-83. doi: 10.1016/j.ejphar.2004.09.006.
34 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.
35 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.
36 Verapamil potentiates anti-glioblastoma efficacy of temozolomide by modulating apoptotic signaling. Toxicol In Vitro. 2018 Oct;52:306-313. doi: 10.1016/j.tiv.2018.07.001. Epub 2018 Jul 9.
37 Inhibition of caspase-dependent mitochondrial permeability transition protects airway epithelial cells against mustard-induced apoptosis. Apoptosis. 2006 Sep;11(9):1545-59. doi: 10.1007/s10495-006-8764-1.
38 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.
39 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
40 Different apoptosis ratios and gene expressions in two human cell lines after sevoflurane anaesthesia. Acta Anaesthesiol Scand. 2009 Oct;53(9):1192-9. doi: 10.1111/j.1399-6576.2009.02036.x. Epub 2009 Jun 30.
41 [Mechanisms underlying the effect of arsenic trioxide on proliferation inhibition and apoptosis induction in myeloma cell line u266]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2007 Oct;15(5):982-5.
42 Lovastatin lactone elicits human lung cancer cell apoptosis via a COX-2/PPAR-dependent pathway. Oncotarget. 2016 Mar 1;7(9):10345-62. doi: 10.18632/oncotarget.7213.
43 Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells. Oncol Res. 2000;12(9-10):397-408. doi: 10.3727/096504001108747855.
44 Comparison of burst of reactive oxygen species and activation of caspase-3 in apoptosis of K562 and HL-60 cells induced by docetaxel. Cancer Lett. 2004 Oct 8;214(1):103-13. doi: 10.1016/j.canlet.2004.03.047.
45 Induction of mitochondrial manganese superoxide dismutase confers resistance to apoptosis in acute myeloblastic leukaemia cells exposed to etoposide. Br J Haematol. 2000 Mar;108(3):574-81. doi: 10.1046/j.1365-2141.2000.01852.x.
46 Cisplatin-enhanced sensitivity of glioblastoma multiforme U251 cells to adenovirus-delivered TRAIL in vitro. Tumour Biol. 2010 Dec;31(6):613-22. doi: 10.1007/s13277-010-0077-x. Epub 2010 Jul 11.
47 Insulin-like growth factor I is the key growth factor in serum that protects neuroblastoma cells from hyperosmotic-induced apoptosis. J Cell Physiol. 2000 Jan;182(1):24-32. doi: 10.1002/(SICI)1097-4652(200001)182:1<24::AID-JCP3>3.0.CO;2-6.
48 mRNA expression analysis of a variety of apoptosis-related genes, including the novel gene of the BCL2-family, BCL2L12, in HL-60 leukemia cells after treatment with carboplatin and doxorubicin. Biol Chem. 2004 Nov;385(11):1099-103. doi: 10.1515/BC.2004.143.
49 Neurokinin-1 receptor (NK1R) inhibition sensitizes APL cells to anti-tumor effect of arsenic trioxide via restriction of NF-B axis: Shedding new light on resistance to Aprepitant. Int J Biochem Cell Biol. 2018 Oct;103:105-114. doi: 10.1016/j.biocel.2018.08.010. Epub 2018 Aug 23.
50 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
51 Effects of gonadotrophin-releasing hormone agonists on apoptosis of granulosa cells. Ann N Y Acad Sci. 2005 May;1042:531-7. doi: 10.1196/annals.1338.065.
52 BMN 673 (talazoparib): A potent PARP inhibitor for triple negative breast cancer with different genetic profile. J Biochem Mol Toxicol. 2019 May;33(5):e22286. doi: 10.1002/jbt.22286. Epub 2019 Jan 23.
53 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
54 Combining kallistatin gene therapy and meloxicam to treat hepatocellular carcinoma in mice. Cancer Sci. 2009 Nov;100(11):2226-33. doi: 10.1111/j.1349-7006.2009.01306.x. Epub 2009 Aug 4.
55 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.
56 Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
57 Expression of the retinoic acid-metabolizing enzyme CYP26A1 limits programmed cell death. Mol Pharmacol. 2005 May;67(5):1808-17. doi: 10.1124/mol.104.005769. Epub 2005 Feb 9.
58 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.
59 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.
60 Role of BAX in the apoptotic response to anticancer agents. Science. 2000 Nov 3;290(5493):989-92. doi: 10.1126/science.290.5493.989.
61 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
62 Mechanisms of thymidine kinase/ganciclovir and cytosine deaminase/ 5-fluorocytosine suicide gene therapy-induced cell death in glioma cells. Oncogene. 2005 Feb 10;24(7):1231-43. doi: 10.1038/sj.onc.1208290.
63 Simvastatin induces apoptosis in human colon cancer cells and in tumor xenografts, and attenuates colitis-associated colon cancer in mice. Int J Cancer. 2008 Aug 15;123(4):951-7. doi: 10.1002/ijc.23593.
64 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
65 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.