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mitotic progression inhibitor
3-Hydroxycapric acid is an inhibitor for mitotic progression. -
Bcl-2 inhibitor
ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). it maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.- Abdel-Aziz S Shatat, .et al. , Purinergic Signal, 2024, May 27 PMID: 38801618
- Tristen Wright, .et al. , Mol Cell, 2024, Apr 4;84(7):1338-1353 PMID: 38503284
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Yibo Wen, .et al. , Ren Fail, 2023, Dec;45(1):2194440 PMID: 37154092
- Rindert Missiaen, .et al. , Cell Metab, 2022, Aug 2;34(8):1151-1167 PMID: 35839757
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Suzuki, Keiji, .et al. , Mutat Res Genet Toxicol Environ Mutagen, 2022, 876-877. 503448
- Rotem Ben-Hamo, .et al. , Nat Commun, 2020, 11: 3296
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Stephanie Ketterer, .et al. , Nat Commun, 2020, Oct 12;11(1):5133 PMID: 33046706
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Min Li, .et al. , Nat Commun, 2020, 11: 4051 PMID: 32792548
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Anderson R, .et al. , EMBO J, 2019, Feb 8. pii: e100492 PMID: 30737259
- Shinya Ishida, .et al. , Oncotarget, 2018, Jun 1; 9(42): 26834-26851 PMID: 29928488
- Rhys Anderson, .et al. , bioRxiv, 2018, 2018
- Ryuta Mikawa, .et al. , Aging Cell, 2018, Oct; 17(5): e12827 PMID: 30058137
- Joo Sang Lee, .et al. , Nat Commun, 2018, 9: 2546 PMID: 29959327
- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Wei TW, .et al. , Cancer Res, 2017, Jan 15;77(2):494-508 PMID: 28069801
- Yusuke Takagi, .et al. , Cancer Sci, 2016, Sep; 107(9): 1270-1280 PMID: 27348272
- Matsumoto M, .et al. , Biochem Biophys Res Commun, 2016, Apr 29;473(2):490-6 PMID: 26996126
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Aloe emodin is a anthraquinone present in aloe latex, an exudate from the aloe plant. It has a strong stimulant-laxative action.
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VEGFR inhibitor
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.- Hasan U, .et al. , Research Square, 2023, 13 Apr
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. , Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Makoto Koyama, .et al. , Int J Oncol, 2020, Sep 2 PMID: 32901840
- Mariko Fujisawa, .et al. , Anticancer Res, 2020, 40: 4445-4455 PMID: 32727774
- Majid Momeny, .et al. , Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. , Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. , Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. , Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738
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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
- Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
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nonsteroidal anti-inflammatory agent
Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. -
p53 activator
JNJ-26854165 is one of p53-activating agents and synergizes with AraC or doxorubicin to induce p53-mediated apoptosis and may provide a novel therapeutic approach for the treatment of acute leukemias.- Chang SJ, .et al. , Arch Biochem Biophys, 2018, Jun 1;647:10-32 PMID: 29655550
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Ubiquitin ligase inducer
Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.- Daniel A. Rauch, .et al. , Retrovirology, 2020, 17: 27 PMID: 32859220
- A Hayano, .et al. , Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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nitroimidazole antibiotic medication
Metronidazole is a nitroimidazole antibiotic medication used particularly for anaerobic bacteria and protozoa. -
Mdm2 antagonist
MDM2 antagonist nutlin-3 is a potent inducer of apoptosis.- Maxime Parisotto, .et al. , J Exp Med, 2018, Jun 4; 215(6): 1749-1763 PMID: 29743291
- Ohmuro-Matsuyama Y, .et al. , Anal Biochem, 2018, Dec 15;563:61-66 PMID: 30316750
- Alisa A. Garaeva, .et al. , Cell Cycle, 2016, 15(1): 64-71 PMID: 26771712
- A G Evstafieva, .et al. , Cell Death Dis., 2014, 5(11): e1511. PMID: 25375376
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Bcl-2 Inhibitor
Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Silva S, .et al. , Sci Rep, 2019, Nov 27;9(1):17703 PMID: 31776405
- Chi-Hung R. Or, .et al. , Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
- P Geserick, .et al. , Cell Death Dis., 2014, 5(9): e1412 PMID: 25210795
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Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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TNF-alpha inhibitor
Pomalidomide is a derivative of thalidomide and acts as an immunomodulator. -
E3 ubiquitin ligase inhibitor
Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo. -
Caspase-1/4 inhibitor
VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.- Joseph Flores, .et al. , Cell Death Dis, 2022, Oct 11;13(10):864 PMID: 36220815
- Arjun Thapa, .et al. , Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. , Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. , Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. , Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. , Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. , J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. , Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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Survivin Inhibitor
YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Ali Nasrollahzadeh, .et al. , Biochim Biophys Acta Mol Cell Res, 2021, Jun 26;1868(10):119087 PMID: 34182011
- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
- Turner TH, .et al. , Sci Rep, 2020, Jan 30;10(1):1493 PMID: 32001757
- Chiou JT, .et al. , Toxicol Appl Pharmacol, 2019, Dec 16;387:114857 PMID: 31837377
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Yamamoto M, .et al. , Anticancer Res, 2019, Feb;39(2):609-617 PMID: 30711936
- Vázquez-Mellado MJ, .et al. , Oncol Rep, 2018, Nov 27 PMID: 30483799
- MASAHIRO YAMAMOTO, .et al. , Anticancer Res, 2018, Dec 38 (12) 6699-6706 PMID: 30504379
- Ahn MR, .et al. , Drug Discov Ther, 2017, 11(6):300-306 PMID: 29332887
- MASAYA MINODA, .et al. , Int J Oncol, 2015, Sep; 47(3): 891-899 PMID: 26166250 t
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Caspase activator
PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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IAP inhibitor
AT-406 is an orally bioavailable inhibitor of IAP family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP).- Yoshikawa M, .et al. , J Med Chem, 2018, Mar 22;61(6):2384-2409 PMID: 29485864
- Tsuyoshi Ishii, .et al. , Sci Rep, 2017, 7: 13000 PMID: 29026104
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MDMX Inhibitor
NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.
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multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
MDM2 inhibitor
Nutlin 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.- Sho Watanabe, .et al. , J Crohns Colitis, 2021, Feb 17 PMID: 33596306
- Shun Zhang, .et al. , BPB Reports, 2019, 2, 130-133
- Momoko Ishimine, .et al. , Dis Markers, 2018, 2018: 5280736 PMID: 29651325
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VEGFR1/2/3/PDGFRβ/Kit/RET/Raf-1 inhibitor
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively. -
anticancer and radioprotection agent
Geniposidic acid is an effective anticancer and radioprotection agent. -
Antagonist of IAPs inhibitor
LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity.- Oliver H, .et al. , J Med Chem, 2023, 66, 16, 11216-11236 PMID: 37535857
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Han-Hee Park, .et al. , Mol Cancer, 2021, Aug 21;20(1):107 PMID: 34419074
- Se-Yeon Park, .et al. , Cell Death & Disease, 2020, 11:744 PMID: 32917855
- J Chen, .et al. , JBC, 2019, June PMID: 31217278
- Choi SW, .et al. , Mol Cell, 2018, Jun 7;70(5):920-935.e7 PMID: 29883609
- Han-Hee Park, .et al. , Exp Mol Med, 2018, Sep; 50(9): 125 PMID: 30237400
- Gi-Bang Koo, .et al. , Cell Res, 2015, Jun; 25(6): 707-725 PMID: 25952668
- Kim SK, .et al. , J Invest Dermatol, 2015, Aug;135(8):2021-2030 PMID: 25748555
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p53 activator
RITA, also referred to as NSC 652287, is a trycyclic thiophene derivative that binds to MDM2, disrupting the MDM2-p53 complex and subsequently activating p53 and inducing apoptosis.- M Kobayashi, .et al. , Oncotarget, 2020, May 5;11(18):1653-1665 PMID: 32405340
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Apoptosis Activator
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells -
RIPK1 inhibitor
Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).- Binjie Yan, .et al. , Cell Death Discov, 2023, 9: 456 PMID: 38097554
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N-SMase inhibitor
GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).
- Guohao Wang, .et al. , Nat Commun, 2021, Sep 30;12(1):5733 PMID: 34593794
- TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
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Bcl-2 inhibitor
Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively. - Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
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TNF inhibitor
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. - Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
- Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
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PINK1 activator
Kinetin riboside is an activator of the Parkinson's Disease-associated PTEN-induced Putative Kinase 1 (PINK1), and acts independently from mitochondrial depolarization. -
miR-544 inhibitor
SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544). -
Caspase/apoptosis activator
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively. -
p53 activator
Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.- Igase M,, .et al. , Exp Cell Res, 2019, Dec 28:111810 PMID: 31891684