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AMPK activator
Acadesine is a selective activator of AMPK in both hepatocytes and adipocytes.
- R. Lim, .et al. , Placenta, 2015, Apr;36(4):454-62 PMID: 25659498
- Stella Liong, .et al. , J Physiol Biochem, 2015, Dec;71(4):703-17 PMID: 26407807
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PARP inhibitor
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- Callum G Jones, .et al. , Cancers (Basel), 2024, Feb 21;16(5):863 PMID: 38473223
- Aurelie Vanderlinden, .et al. , Br J Cancer, 2023, Nov;129(11):1829-1840 PMID: 37777579
- Saptarshi Sinha, .et al. , Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. , Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. , Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. , Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. , Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. , Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. , DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. , Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. , Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. , J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. , Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. , Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. , Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (T. wilfordii). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of α-tocopherol.
- Xuechun Wang, .et al. , Int J Mol Sci, 2023, Mar 8;24(6):5204 PMID: 36982279
- R. San Gil, .et al. , bioRxiv, 2020, Jan
- Abdin AA, .et al. , Eur J Pharmacol., 2014, 742:102-12 PMID: 25218987
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Bcl-2 Inhibitor
ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).- Jung Mo Lee, .et al. , Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. , Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. , Med, 2021, 2,1-13
- Ying Ji, .et al. , Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. , Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. , Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. , Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. , Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. , J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. , Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. , Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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glucocorticoid receptor agonist
Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant. Its potency is about 20-30 times that of the naturally occurring hormone hydrocortisone and 4-5 times of prednisone.- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Topoisomerase II inhibitor
Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.- Wan J. Gan, .et al. , bioRxiv, 2024, March 10
- Zoya Mann, .et al. , Mol Biol Cell, 2024, Jan 1; 35(1) PMID: 37903230
- Bageshri Naimish Nanavati, .et al. , bioRxiv, 2023, Feb 23 PMID: 36865131
- Sibei Wang, .et al. , Molecules, 2023, Jan 19;28(3):1016 PMID: 36770683
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- Metformin hydrochloride is a biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.
- Matthew A Schaller, .et al. , JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. , bioRxiv, 2021, January 21
- Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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HMG-CoA reductase inhibitor
Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis.- Weizhen Chen, .et al. , Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. , Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. , J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. , Sci Rep, 2017, 7: 8090 PMID: 28808351
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PLA inhibitor
Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.- Darshika Pathiraja, .et al. , Food Chem, 2023, May 1;407:135145 PMID: 36521391
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mTOR Inhibitor
PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.- Nobuyuki Kondo, .et al. , JCI Insight, 2023, Dec 22;8(24):e173688 PMID: 37917191
- Hiroshi Fukamachi, .et al. , J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Fuse MJ, .et al. , Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
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MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. - Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases???LOX, IC50=2.7 μM???, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects.
- Wafa Naji Shnaikat, .et al. , Iraqi J Pharm Sci, 2023, 31(Suppl.):92-99
- Ha T. Tran, .et al. , PLoS One, 2017, 12(3): e0173373 PMID: 28278187
- Salidroside (Rhodioloside) is a glucoside of tyrosol found in the plant Rhodiola rosea. It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin.
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HMG-CoA reductase inhibitor
Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM. -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
RTK inhibitor
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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MEK inhibitor
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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HDAC inhibitor
Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.- Amy E Neely, .et al. , Commun Biol, 2023, Jun 23;6(1):664 PMID: 37353594
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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JAK1/2 Inhibitor
INCB018424 is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively;- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. , Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. , Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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PDGFR/FLT3 Inhibitor
Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Autophagy/PI3K Inhibitor
3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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Protein translocation Inhibitor
Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange. -
JAK1/2 inhibitor
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. -
JAK inhibitor
Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. - Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties.
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Mitochondrial respiratory chain inhibitor
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. -
HMG-CoA reductase inhibitor
Pitavastatin Lactone is an HMG-CoA reductase inhibitor. -
DRP1 inhibitor
Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.- Umut Kerem Kolac, .et al. , Mol Biol Rep, 2023, Jan;50(1):493-506 PMID: 36352179
- KOLAC UK, .et al. , Research Square, 2022, 03 Jun
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Topoisomerase II inhibitor
Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.- Laura Wiggins, .et al. , Nat Commun, 2023, 14: 1854
- Stefania Scialla, .et al. , Int J Pharm, 2023, Feb 5;632:122575 PMID: 36603672
- Fernando Espinola-Portilla, .et al. , Mol. Pharmaceutics, 2023, 20(3): 1490-1499
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- R Mahalakshmi, .et al. , Mol Biol Rep, 2022, Jan;49(1):463-476 PMID: 34739690
- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
- Abdelrehim A, .et al. , PLoS One, 2019, Feb 22;14(2):e0212701 PMID: 30794671
- J Wei, .et al. , bioRxiv, 2018, 2018
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JAK inhibitor
S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor. -
glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. - Mitochonic Acid 5 is a derivative of the plant hormone indole-3-acetic acid.
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glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
HDAC inhibitor
Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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multi-targeted receptor tyrosine kinase inhibitor
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
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glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
mitophagy regulator
P62-mediated mitophagy inducer is a mitophagy regulator which activates mitophagy without recruiting Parkin or collapsing δ??m and retains activity in cells devoid of a fully functional PINK1/Parkin pathway. - Urolithin A, a gut-microbial metabolite of ellagic acid, exerts anti-inflammatory, antiproliferative, and antioxidant properties. Urolithin A induces autophagy and apoptosis, suppresses cell cycle progression, and inhibits DNA synthesis.
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AMP-activated protein kinase activator
AICAR phosphate is an activator of AMP-activated protein kinase (AMPK). -
autophagy/mitophagy inhibitor
Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc. -
antiviral agent
cis-Resveratrol exhibits signifcant antiviral activity. cis-Resveratrol inhibits enteroviruses with IC50s of 12.2 ?M and 37.6 ?M for coxsackievirus B3 (CVB3) and enterovirus 71 (EV71), respectively.