General Information of Drug (ID: DMCQUWI)

Drug Name
PI-3065 Drug Info
Synonyms PI 3065
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
24937012
ChEBI ID
CHEMBL4450504
TTD Drug ID
DMCQUWI

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug(s) Targeting PI3-kinase beta (PIK3CB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Buparlisib DM1WEHC Breast cancer 2C60-2C65 Phase 3 [3]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [4]
PA-799 DMLSYJQ Colorectal cancer 2B91.Z Phase 1/2 [5]
AZD8186 DMWYF1H Solid tumour/cancer 2A00-2F9Z Phase 1 [6]
GSK2636771 DMCBGLW Prostate cancer 2C82.0 Phase 1 [7]
BAY 1082439 DMLRGX1 Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
AZD6482 DMVP4E5 Thrombosis DB61-GB90 Terminated [9]
PP121 DMU8KTO Discovery agent N.A. Investigative [10]
PIK-75 DM9BQTX Discovery agent N.A. Investigative [11]
KU-0060648 DMQWS6U Discovery agent N.A. Investigative [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting PI3-kinase gamma (PIK3CG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [13]
IPI-145 DMWA24P Follicular lymphoma 2A80 Approved [14]
Buparlisib DM1WEHC Breast cancer 2C60-2C65 Phase 3 [3]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [15]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [16]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [15]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [17]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [18]
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [18]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [19]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [20]
Gefitinib DM15F0X Colon adenocarcinoma Approved [21]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [22]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [23]
Etretinate DM2CZFA Keratosis ED56 Approved [24]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [25]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [26]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [27]
Quercetin DM3NC4M Obesity 5B81 Approved [28]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [29]
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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 [30]
Gefitinib DM15F0X Colon adenocarcinoma Approved [31]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [32]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [23]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [33]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [34]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [33]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [35]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [36]
Methotrexate DM2TEOL Anterior urethra cancer Approved [37]
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Drug(s) Affected By Cadherin-1 (CDH1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [38]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [39]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [40]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [41]
Liraglutide DM3FXPS Non-insulin dependent diabetes 5A11 Approved [42]
Quercetin DM3NC4M Obesity 5B81 Approved [43]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [44]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [45]
Polyethylene glycol DM4I1JP Constipation DD91.1 Approved [46]
Panobinostat DM58WKG Chronic graft versus host disease Approved [47]
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Drug(s) Affected By Cadherin-2 (CDH2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [48]
Quercetin DM3NC4M Obesity 5B81 Approved [43]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [49]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [50]
Panobinostat DM58WKG Chronic graft versus host disease Approved [47]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [51]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [52]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [53]
Testosterone DM7HUNW Hot flushes GA30 Approved [54]
Acocantherin DM7JT24 Atrial fibrillation BC81.3 Approved [55]
⏷ 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 [56]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [48]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [57]
Methotrexate DM2TEOL Anterior urethra cancer Approved [58]
Quercetin DM3NC4M Obesity 5B81 Approved [59]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [45]
Levamisole DM5EN79 Parasitic infection 1D0Y-1G2Z Approved [60]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [61]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [62]
Promethazine DM6I5GR Hyperemesis gravidarum Approved [63]
⏷ 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
PI3-kinase beta (PIK3CB) TTTHBCA PK3CB_HUMAN Inhibitor [1]
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Inhibitor [1]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Baculoviral IAP repeat-containing protein 5 (BIRC5) OTILXZYL BIRC5_HUMAN Gene/Protein Processing [2]
Bcl-2 homologous antagonist/killer (BAK1) OTDP6ILW BAK_HUMAN Gene/Protein Processing [2]
Cadherin-1 (CDH1) OTFJMXPM CADH1_HUMAN Gene/Protein Processing [2]
Cadherin-2 (CDH2) OTH0Y56P CADH2_HUMAN Gene/Protein Processing [2]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Protein Interaction/Cellular Processes [2]
Vimentin OTGZLW4J VIME_HUMAN Gene/Protein Processing [2]

References

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2 PI3K inhibitor PI-3065 induces apoptosis in hepatocellular carcinoma cells by targeting survivin. Chem Biol Interact. 2023 Feb 1;371:110343. doi: 10.1016/j.cbi.2023.110343. Epub 2023 Jan 6.
3 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
4 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: 2154).
5 The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
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8 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
9 Human target validation of phosphoinositide 3-kinase (PI3K)beta: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kbeta inhibitor. J Thromb Haemost. 2012 Oct;10(10):2127-36.
10 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
11 Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007 Sep 1;15(17):5837-44.
12 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity. J Med Chem. 2013 Aug 22;56(16):6386-401.
13 BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
14 PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
16 Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
17 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: 2155).
18 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: 2156).
19 An integrin-targeted, pan-isoform, phosphoinositide-3 kinase inhibitor, SF1126, has activity against multiple myeloma in vivo.Cancer Chemother Pharmacol.2013 Apr;71(4):867-81.
20 mTOR inhibition reverses acquired endocrine therapy resistance of breast cancer cells at the cell proliferation and gene-expression levels. Cancer Sci. 2008 Oct;99(10):1992-2003. doi: 10.1111/j.1349-7006.2008.00955.x.
21 Leptomycin B reduces primary and acquired resistance of gefitinib in lung cancer cells. Toxicol Appl Pharmacol. 2017 Nov 15;335:16-27. doi: 10.1016/j.taap.2017.09.017. Epub 2017 Sep 21.
22 Assessment of the cytotoxic, genotoxic, and apoptotic potential of flurbiprofen in HeLa and HepG2 cell lines. J Biochem Mol Toxicol. 2021 Jun;35(6):1-11. doi: 10.1002/jbt.22770. Epub 2021 Mar 11.
23 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.
24 Bexarotene activates the p53/p73 pathway in human cutaneous T-cell lymphoma. Br J Dermatol. 2009 Mar;160(3):519-26. doi: 10.1111/j.1365-2133.2008.08931.x. Epub 2008 Nov 25.
25 Expression profile analysis of colon cancer cells in response to sulindac or aspirin. Biochem Biophys Res Commun. 2002 Mar 29;292(2):498-512.
26 Apoptotic induction by simvastatin in human lung cancer A549 cells via Akt signaling dependent down-regulation of survivin. Invest New Drugs. 2011 Oct;29(5):945-52. doi: 10.1007/s10637-010-9450-2. Epub 2010 May 13.
27 Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. Oncogene. 2005 Sep 15;24(41):6213-21. doi: 10.1038/sj.onc.1208774.
28 Quercetin inhibit human SW480 colon cancer growth in association with inhibition of cyclin D1 and survivin expression through Wnt/beta-catenin signaling pathway. Cancer Invest. 2009 Jul;27(6):604-12. doi: 10.1080/07357900802337191.
29 Troglitazone sensitizes tumor cells to TRAIL-induced apoptosis via down-regulation of FLIP and Survivin. Apoptosis. 2006 Sep;11(9):1503-12. doi: 10.1007/s10495-006-8896-3.
30 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.
31 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.
32 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.
33 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.
34 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.
35 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.
36 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
37 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.
38 Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
39 Manganese superoxide dismutase induces migration and invasion of tongue squamous cell carcinoma via H2O2-dependent Snail signaling. Free Radic Biol Med. 2012 Jul 1;53(1):44-50. doi: 10.1016/j.freeradbiomed.2012.04.031. Epub 2012 May 9.
40 Nitric oxide causes anoikis through attenuation of E-cadherin and activation of caspase-3 in human gastric carcinoma AZ-521 cells infected with Mycoplasma hyorhinis. J Vet Med Sci. 2010 Jul;72(7):869-74.
41 Induced differentiation in HT29, a human colon adenocarcinoma cell line. J Cell Sci. 1999 Aug;112 ( Pt 16):2657-66. doi: 10.1242/jcs.112.16.2657.
42 Antitumoral activity of liraglutide, a new DNMT inhibitor in breast cancer cells in vitro and in vivo. Chem Biol Interact. 2021 Nov 1;349:109641. doi: 10.1016/j.cbi.2021.109641. Epub 2021 Sep 14.
43 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.
44 Troglitazone increases expression of E-cadherin and claudin 4 in human pancreatic cancer cells. Biochem Biophys Res Commun. 2009 Mar 13;380(3):614-9. doi: 10.1016/j.bbrc.2009.01.134. Epub 2009 Jan 27.
45 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
46 Regulation of epithelial cell morphology and functions approaching to more in vivo-like by modifying polyethylene glycol on polysulfone membranes. PLoS One. 2012;7(4):e36110.
47 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
48 Microarray analysis of H2O2-, HNE-, or tBH-treated ARPE-19 cells. Free Radic Biol Med. 2002 Nov 15;33(10):1419-32.
49 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
50 Effects of all-trans and 9-cis retinoic acid on differentiating human neural stem cells in vitro. Toxicology. 2023 Mar 15;487:153461. doi: 10.1016/j.tox.2023.153461. Epub 2023 Feb 16.
51 Arsenic trioxide inhibits EMT in hepatocellular carcinoma by promoting lncRNA MEG3 via PKM2. Biochem Biophys Res Commun. 2019 Jun 11;513(4):834-840. doi: 10.1016/j.bbrc.2019.04.081. Epub 2019 Apr 16.
52 Thalidomide suppresses angiogenesis and immune evasion via lncRNA FGD5-AS1/miR-454-3p/ZEB1 axis-mediated VEGFA expression and PD-1/PD-L1 checkpoint in NSCLC. Chem Biol Interact. 2021 Nov 1;349:109652. doi: 10.1016/j.cbi.2021.109652. Epub 2021 Sep 11.
53 ?9-tetrahydrocannabinol inhibits epithelial-mesenchymal transition and metastasis by targeting matrix metalloproteinase-9 in endometrial cancer. Oncol Lett. 2018 Jun;15(6):8527-8535. doi: 10.3892/ol.2018.8407. Epub 2018 Apr 2.
54 Anti-androgen 2-hydroxyflutamide modulates cadherin, catenin and androgen receptor phosphorylation in androgen-sensitive LNCaP and androgen-independent PC3 prostate cancer cell lines acting via PI3K/Akt and MAPK/ERK1/2 pathways. Toxicol In Vitro. 2017 Apr;40:324-335. doi: 10.1016/j.tiv.2017.01.019. Epub 2017 Feb 2.
55 Ouabain impairs cell migration, and invasion and alters gene expression of human osteosarcoma U-2 OS cells. Environ Toxicol. 2017 Nov;32(11):2400-2413. doi: 10.1002/tox.22453. Epub 2017 Aug 10.
56 Increased expression of VDAC1 sensitizes carcinoma cells to apoptosis induced by DNA cross-linking agents. Biochem Pharmacol. 2012 May 1;83(9):1172-82. doi: 10.1016/j.bcp.2012.01.017. Epub 2012 Jan 21.
57 Sulindac-derived reactive oxygen species induce apoptosis of human multiple myeloma cells via p38 mitogen activated protein kinase-induced mitochondrial dysfunction. Apoptosis. 2007 Jan;12(1):195-209. doi: 10.1007/s10495-006-0527-5.
58 Functional gene expression profile underlying methotrexate-induced senescence in human colon cancer cells. Tumour Biol. 2011 Oct;32(5):965-76.
59 Inhibition of lung cancer cell growth by quercetin glucuronides via G2/M arrest and induction of apoptosis. Drug Metab Dispos. 2006 Feb;34(2):296-304. doi: 10.1124/dmd.105.005280. Epub 2005 Nov 9.
60 Levamisole induced apoptosis in cultured vascular endothelial cells. Br J Pharmacol. 2000 Dec;131(8):1577-83.
61 Arsenic trioxide (As(2)O(3)) induced apoptosis and its mechanisms in a human esophageal squamous carcinoma cell line. Chin Med J (Engl). 2002 Feb;115(2):280-5.
62 Non-steroidal anti-inflammatory drugs induce apoptosis in gastric cancer cells through up-regulation of bax and bak. Carcinogenesis. 2001 Sep;22(9):1393-7. doi: 10.1093/carcin/22.9.1393.
63 AMPK activation induced by promethazine increases NOXA expression and Beclin-1 phosphorylation and drives autophagy-associated apoptosis in chronic myeloid leukemia. Chem Biol Interact. 2020 Jan 5;315:108888. doi: 10.1016/j.cbi.2019.108888. Epub 2019 Nov 2.