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XIAP/cIAP1 antagonist
Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.- Antonella Antignani, .et al. , FASEB J, 2023, Dec;37(12):e23292 PMID: 37971407
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cIAP-2 antagonist
SM-164 is a potent cell-permeable and bivalent Smac mimetic which bind to a XIAP protein with a Ki value of 0.56 nM, and binds to cIAP-1 and cIAP-2 proteins with Ki values of 0.31 and 1.1 nM, respectively.- Antonella Antignani, .et al. , FASEB J, 2023, Dec;37(12):e23292 PMID: 37971407
- Hanna Yuk, .et al. , Antioxidants (Basel), 2021, Aug 25;10(9):1347 PMID: 34572979
- Caroline Moerke, .et al. , Cell Death Differ, 2018, Nov 15 PMID: 30442947
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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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Survivin Inhibitor
YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.- Atieh Pourbagheri-Sigaroodi, .et al. , Iran J Allergy Asthma Immunol, 2024, 23(6):699-726 PMID: 39985496
- 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
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Caspase inhibitor
Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).- Baosen Jia, .et al. , Nature, 2026, Apr;652(8112):1362-1374 PMID: 42020739
- Andrew Kent, .et al. , Nat Immunol, 2025, Jan;26(1):53-67 PMID: 39747433
- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Davide Pradella, .et al. , Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. , Cell Death Differ, 2020, Feb 3 PMID: 32015503
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HO-1 inhibitor
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
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Caspase-1 inhibitor
Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.- Binjie Yan, .et al. , Cell Death Discov, 2023, 9: 456 PMID: 38097554
- Yuping Fan, .et al. , Sci Transl Med, 2021, Jul 28;13(604):eabb1069 PMID: 34321317
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NF-κB inhibitor
QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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PERK inhibitor
GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Linhao Xu, .et al. , Neural Plasticity, 2021, 23 Aug PMID: 34471408
- Takashi Shimizu, .et al. , Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
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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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RIPK1 inhibitor
Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).- Cheng Chen, .et al. , Neurochem Res, 2025, Mar 18;50(2):122 PMID: 40100474
- Binjie Yan, .et al. , Cell Death Discov, 2023, 9: 456 PMID: 38097554
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Bcl-2 inhibitor
ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.- Christina Mayerhofer, .et al. , Cell Metabolism, 2025, 37(10): 2014-2029 PMID: 40961937
- Yasharah Raza, .et al. , bioRxiv, 2025, Jan 22:2025.01.19.633759 PMID: 39896667
- Kam Pui Tam, .et al. , PLoS Pathog, 2024, Sep 26;20(9):e1012250 PMID: 39325843
- Lindy Vernooij, .et al. , EJC Paediatric Oncology, 2024, 3: 100168
- Tristen Wright, .et al. , Mol Cell, 2024, Apr 4;84(7):1338-1353 PMID: 38503284
- Dilay Karademir, .et al. , Med Oncol, 2023, Jul 11;40(8):234 PMID: 37432531
- Nageswara Rao Reddy, .et al. , Bioanalysis, 2022, Mar;14(5):253-266 PMID: 35172610
- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
- Anna L Koessinger, .et al. , Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. , Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Martin Grundy, .et al. , PLoS One, 2018, 13(1): e0190682 PMID: 29298347
- Joanne Dai, .et al. , J Immunol, 2018, 200 (5) 1727-1736 PMID: 29358277
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Bcl-2 inhibitor
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.- Christopher D. Graham, .et al. , Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
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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.- Da-Hye Jeong, .et al. , Adv Sci (Weinh), 2025, Apr;12(13):e2412393 PMID: 39921454
- 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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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.- Ella Martin, .et al. , ACS Pharmacol Transl Sci, 2025, May 12;8(9):2996-3006 PMID: 40969890
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eIF2α dephosphorylation inhibitor
Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).- Gregory R. Kardos, .et al. , Front Oncol, 2020, 10: 834 PMID: 32637352
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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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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
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p53 Inhibitor
Pifithrin-beta is a small molecule inhibitor of p53.- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
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Caspase-3 inhibitor
Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
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caspase 8 inhibitor
Z-IETD-FMK is a specific inhibitor of caspase 8.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
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Caspase-9 Inhibitor
Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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PERK Inhibitor
GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC(50) of 0.9 nmol/L. It is highly selective for PERK with IC(50) values >100 nmol/L against a panel of 300 kinases.- Jun Liu, .et al. , Food Chem, 2023, Jun 30;412:135550 PMID: 36706507
- Cao W, .et al. , J Cell Mol Med, 2019, Aug 23 PMID: 31441588
- Kosuke Ishikawa, .et al. , Biology Methods and Protocols, 2018, 1-10 PMID: 32161797
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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 PMID: 34617070
- 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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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.- Kazuya Ishiguro, .et al. , Cancer Lett, 2025, Oct 28:631:217941 PMID: 40701319
- Sumie Fujii, .et al. , Stem Cells and Development, 2025, 34: 9-10 PMID: 40130551
- 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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IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
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Mdm2 inhibitor
YH239-EE is a potent p53-MDM2 antagonist and an apoptosis inducer.- Kim, Y, .et al. , Cells, 2026, 15(5):473 PMID: 41827906
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N-SMase inhibitor
GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).
- Laozhi Xie, .et al. , ACS Nano, 2026, Jun 23;20(24):17442-17462 PMID: 42249854
- Salar Ghaffari Gabaran, .et al. , Biochem Pharmacol, 2025, Sep:239:117019 PMID: 40499840
- Guohao Wang, .et al. , Nat Commun, 2021, Sep 30;12(1):5733 PMID: 34593794
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PERK inhibitor
ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM.- Le Xu, .et al. , Cell Stem Cell, 2024, Aug 16:S1934-5909(24)00287-X PMID: 39181129
- SeungHye Han, .et al. , Nature, 2023, Aug;620(7975):890-897 PMID: 37558881
- Zhou W, .et al. , Research Square, 2023, MAY 03
- Satoshi Watanabe, .et al. , Proc Natl Acad Sci U S A, 2021, May 18;118(20) PMID: 33972447
- Satoshi Watanabe, .et al. , bioRxiv, 2020, February 27
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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.- Lila Louadj, .et al. , Sci Rep, 2026, Apr 4;16(1):16233 PMID: 41935207
- Uzma Hasan, .et al. , Drug Deliv Transl Res, 2024, Feb;14(2):342-359 PMID: 37587289
- 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 PMID: 32593665
- 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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MDM2 degrader
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.- Lingling Chen, .et al. , Biochem Pharmacol, 2024, Nov 29:232:116688 PMID: 39617210
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ASK1 inhibitor
Selonsertib is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.- Lisa M Kim, .et al. , Cancer Res, 2022, Sep 2;82(17):3045-3057 PMID: 35792658
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
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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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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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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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Caspase-3 Inhibitor
Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.- Megumi Andoh, .et al. , Nat Commun, 2025, Jan 22;16(1):918 PMID: 39843445
- Geoffrey Canet, .et al. , Res Sq, 2024, May 14:rs.3.rs-4384494 PMID: 38798432
- Roi Ankawa, .et al. , Dev Cell, 2021, Jul 12;56(13):1900-1916 PMID: 34197726
- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
- Akashi E, .et al. , Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
- Wenquan Liang, .et al. , Sci Rep, 2016, 6: 38267 PMID: 27905569
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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.- Mikako Hirose, .et al. , Biosci Biotechnol Biochem, 2025, Dec 18;90(1):76-87 PMID: 41134023
- Song Han, .et al. , Neoplasia, 2025, Jan:59:101070 PMID: 39541736
- 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 PMID: 35483779
- Rotem Ben-Hamo, .et al. , Nat Commun, 2020, 11: 3296 PMID: 32620799
- 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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GPX4 inhibitor
ML-210??the most potent compound in the nitroisoxazole series?? is a selective covalent inhibitor of glutathione peroxidase 4 (GPX4) by binding the selenocysteine residue.- Ning Li, .et al. , J Ovarian Res, 2024, Feb 23;17(1):49 PMID: 38396022
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Pan Caspase Inhibitor
Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.- Perla Nafeh, .et al. , BMC Complement Med Ther, 2025, Aug 13;25(1):304 PMID: 40804627
- Cheng Chen, .et al. , Neurochem Res, 2025, Mar 18;50(2):122 PMID: 40100474
- Lara Ebbert, .et al. , Antioxidants (Basel), 2024, Jul; 13(7): 864 PMID: 39061932
- Rushikesh Deshpande, .et al. , Int J Mol Sci, 2024, Jan 18;25(2):1157 PMID: 38256231
- Sarah Metcalfe, .et al. , J Leukoc Biol, 2023, Jul 27;qiad089 PMID: 37497744
- Kazutoshi Toriyama, .et al. , Oncol Lett, 2023, Nov 10;27(1):12 PMID: 38028184
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Akira Endo, .et al. , Dev Cell, 2023, Oct 9;58(19):1819-1829 PMID: 37716356
- Rui Zhou, .et al. , Nagoya J Med Sci, 2023, Aug;85(3):579-591 PMID: 37829490
- Chantal-Kristin Wenzel, .et al. , Toxicol In Vitro, 2023, Sep;91:105625 PMID: 37268255
- Joshua H Choe, .et al. , Cancer Discov, 2023, May 4;13(5):1250-1273 PMID: 37067901
- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
- Debin Qi, .et al. , Cell Cycle, 2023, Apr;22(7):818-828 PMID: 36482709
- Ming-Chun Hung, .et al. , Cell Biosci, 2022, 12: 122 PMID: 35918763
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MDMX inhibitor
SJ 172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified.- Saketh S Dinavahi, .et al. , Cancer Immunol Res, 2022, Jun 3;10(6):757-769 PMID: 35439317
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HDAC inhibitor
Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.- Satoshi Endo, .et al. , J Biochem, 2021, Mar 17 PMID: 33729485
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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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Caspase inhibitor
Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models.- Sohya Fujimoto, .et al. , Cells, 2025, Mar 27;14(7):498 PMID: 40214452
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Bax channel blocker
Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).- Stella Victorelli, .et al. , Nature, 2023, Oct;622(7983):627-636 PMID: 37821702
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Bax activator
BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX.- Takino JI, .et al. , Sci Rep, 2019, Nov 13;9(1):16717 PMID: 31723205
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Bcl-2 Inhibitor
Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively).- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- 5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity.
- Tz-Feng Lin, .et al. , Mater Today Commun, 2022, 33: 104284
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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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MCL-1 inhibitor
A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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BCL-XL inhibitor
A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki = <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM)- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805

