-
PARP inhibitor
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.- 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
-
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
-
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.- 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
-
autophagy inhibitor
Monensin sodium is an ionophore and inhibitor of autophagy commercially used in livestock feed. It inhibits autophagy, interfering with the fusion of the autophagosome and the lysosome. -
ALK Inhibitor
TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).- Yue Guo, .et al. , Cell Biosci, 2022, Dec 30;12(1):210 PMID: 36585695
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
-
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
-
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
-
mTOR Inhibitor
PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.- 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
-
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. -
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).- 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
-
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
-
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
-
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;- 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
-
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
-
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
-
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. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
LRRK2 kinase inhibitor
GSK2578215A is a potent leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively). -
LRRK2 Inhibitor III
HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2. -
Autophagy Inhibitor
Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
-
LRRK2 inhibitor
CZC-25146 is a potent and selective LRRK2 inhibitor. CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency. -
LRRK2 inhibitor
GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
-
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
-
Glutaminase inhibitor
CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.
- Beatriz Giesen, .et al. , Pharmaceutics, 2021, Feb 23;13(2):295 PMID: 33672398
-
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
-
JAK inhibitor
S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor. -
LRRK2 inhibitor
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC50 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively. -
ULK1 inhibitor
SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .- SR Bonam, .et al. , Cells, 2020, May; 9(5): 1321 PMID: 32466347
- Altea Rocchi, .et al. , PLoS Genet, 2017, Aug; 13(8): e1006962 PMID: 28806762
-
Autophagy inhibitor
Lys05 is a potent lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. -
Autophagy inhibitor
Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34. -
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
-
CoA reductase inhibitor
Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor. -
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.- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
-
ULK1/ULK2 inhibitor
MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively. -
lysosomal autophagy inhibitor
Lys01 trihydrochloride (Lys05) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay. -
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.