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Bcl-2 inhibitor
ABT-263，也被称为 Navitoclax，是一种强效且可口服的 Bcl-2家族抑制剂（对Bcl-2、Bcl-xL和Bcl-w的Ki值<1 nmol/L）。它对Bcl-xL、Bcl-2和Bcl-w具有高亲和力（Ki ≤1 nmol/L），但对Mcl-1和A1的结合能力较弱。- 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
- 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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VEGFR inhibitor
Regorafenib（BAY 73-4506）是一种多激酶抑制剂，其IC50分别为17、40和69 nM的c-KIT、VEGFR2、B-Raf。Regorafenib（BAY 73-4506）是一种口服生物可用的多激酶抑制剂，针对肿瘤及其血管系统。- 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 是一种广谱 Bcl-2 抑制剂。IC50 值从 192 nM（前B细胞系 Hal-01）到小于 10 μM（Nalm-6、K562 和 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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Bcl-2 Inhibitor
Bcl-2同源结构域-3（BH3）拟态剂，可拮抗所有抗凋亡的Bcl-2家族蛋白（平均IC50为3微摩尔/升），包括Mcl-1（IC50为2.9微摩尔/升）和Bfl-1（IC50为5微摩尔/升）。- 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) 是一种针对 Aurora A/B/C 的 Aurora 激酶抑制剂，在无细胞试验中的 IC50 分别为 13 nM/79 nM/61 nM，对 Abl、TrkA、c-RET 和 FGFR1 有适度的抑制效力，对 Lck、VEGFR2/3、c-Kit、CDK2 等的抑制效力较低。目前处于临床试验第二阶段。- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Caspase-1/4 inhibitor
VX-765 是一种新型的 Caspase-1 抑制剂，这是一种控制两种细胞因子，IL-1b 和 IL-18 生成的酶。- 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 是一种新型小分子 survivin 抑制剂，其对 survivin 启动子活性的抑制 IC50 为 0.54 nM。- Atieh Pourbagheri-Sigaroodi, .et al. , Iran J Allergy Asthma Immunol, 2024, 23(6):699-726
- 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
- V??zquez-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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IAP inhibitor
AT-406 是一种口服生物可用的 IAP家族蛋白 抑制剂，具有潜在的诱导凋亡和抗肿瘤活性。AT-406 选择性地抑制 IAP蛋白 的生物活性，包括 X染色体连锁IAP（XIAP）、细胞IAPs 1（c-IAP1）和2（c-IAP2）以及黑色素瘤凋亡抑制蛋白（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 是一种细胞渗透性的苯并呋喃化合物，它通过抑制 MDMX 启动子的转录活性（在 HT1080 细胞中的 IC50 = 2.5 微摩尔），在 MCF-7、LNCaP 和 A549 细胞中（1 到 10 微摩尔，持续 16 到 24 小时）降低 p53 负调控因子 MDMX 蛋白的水平，从而增强 p53 的稳定性和激活。 -
multi-kinase inhibitor
Lestaurtinib（CEP-701；KT-5555）是一种多激酶抑制剂，对Trk家族的受体酪氨酸激酶具有强大的活性。Lestaurtinib抑制JAK2、FLT3和TrkA的IC50分别为0.9、3和小于25 nM。 -
MDM2 inhibitor
Nutlin 3a 是一种强效的 MDM2 (mouse double minute 2) 抑制剂，它能阻止 MDM2 与 p53 的结合，从而诱导 p53 调控基因的表达，并在表达功能性 p53 的细胞中显示出强大的抗增殖活性。- 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 是一种多靶点抑制剂，针对 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1，其半抑制浓度（IC50）分别为 13/4.2/46、22、7、1.5 和 2.5 纳摩尔 (nM)。 -
RIPK1 inhibitor
Necrostatin-1 是一种 ATP 竞争性的、变构抑制剂，针对受体相互作用蛋白激酶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 是一种细胞渗透性、选择性的 N-SMase (中性鞘磷脂酶) 抑制剂。- Guohao Wang, .et al. , Nat Commun, 2021, Sep 30;12(1):5733 PMID: 34593794
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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. -
Pan Caspase Inhibitor
Z-VAD-FMK 是一种细胞渗透性、不可逆的全泛凋亡酶抑制剂。在体外实验中，能够抑制肿瘤细胞中的凋亡酶加工和凋亡诱导（IC50 = 0.0015 - 5.8 mM）。在体内也显示活性。- 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
- Kaori Kanemaru, .et al. , Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. , Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. , Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. , Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. , Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Simon Boudreault, .et al. , Viruses, 2022, Dec 3;14(12):2710 PMID: 36560714
- Kosar Jabbari, .et al. , Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. , Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. , Apoptosis, 2021, Apr 27 PMID: 33905036
- Hideyuki Kinoshita, .et al. , Anticancer Res, 2021, Dec;41(12):6013-6021 PMID: 34848455
- Sofia Giacosa, .et al. , Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hideyuki Kinoshita, .et al. , Anticancer Res, 2021, Oct;41(10):4947-4955 PMID: 34593442
- Hannes Schmid, .et al. , Haematologica, 2021, Jan 14 PMID: 33440919
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- El-Ashmawy NE, .et al. , Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. , Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. , Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. , Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. , J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. , Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. , Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. , Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. , J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. , Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. , Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. , Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. , Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. , Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. , Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. , Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. , J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. , Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
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PKD inhibitor
CID 2011756 是一种蛋白激酶 D（PKD）抑制剂（IC50 值分别为 PKD2、PKD3 和 PKD1 的 0.6、0.7 和 3.2 μM）。 -
PKD inhibitor
kb NB 142-70 是一种选择性的蛋白激酶D（PKD）抑制剂（IC50值分别为PKD1、2和3的28.3、58.7和53.2 nM）。 -
p53 Inhibitor
Pifithrin-beta 是一种小分子p53抑制剂。- J Priyanga, .et al. , Chem Biol Interact, 2020, Nov 1;331:109250 PMID: 32956706
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p53 inhibitor
Pifithrin-α hydrobromide 是一种可逆的 p53 介导的凋亡和 p53 依赖的基因转录抑制剂，如 cyclin G、p21/waf1 和 mdm2 的表达。 -
Bcl-2 inhibitor
ABT-199 是一种所谓的 BH3-拟态药物，旨在阻断 Bcl-2 蛋白 的功能。- 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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Caspase-6 inhibitor
Z-VEID-FMK 是caspase-6/Mch2的特异性识别序列。Z-VEID-FMK 是一种合成肽，可以不可逆地抑制依赖VEID的caspases（例如，caspase-6）的活性。该抑制剂被设计为甲酯形式，以便于细胞渗透。 -
Caspase-2 inhibitor
Z-VDVAD-FMK 是一种细胞渗透性的、不可逆的caspase-2抑制剂。caspase抑制剂在研究生物过程中扮演着重要角色。 -
eIF2α dephosphorylation inhibitor
Salubrinal 是一种细胞渗透性、选择性抑制剂，专门抑制细胞内磷酸酶复合体，这些复合体会去磷酸化真核翻译起始因子2亚基α（eIF2α）。它能保护细胞免受内质网应激诱导的凋亡（EC50 约为 15 μM）。- Gregory R. Kardos, .et al. , Front Oncol, 2020, 10: 834 PMID: 32637352
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Caspase-3 inhibitor
Z-DQMD-FMK 是一种合成肽，可以不可逆地抑制 Caspase-3 的活性。- Jason Segura, .et al. , PLoS One, 2023, Feb 13;18(2):e0281087 PMID: 36780482
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NF-κB inhibitor
QNZ 抑制转录因子 NF-κB 的激活，并已用于研究 NF-κB 信号传导。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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PERK inhibitor
GSK2606414 是一种口服可用的、高效的、选择性的 PERK 抑制剂，IC50 为 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
- Takashi Shimizu, .et al. , Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
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caspase 8 inhibitor
Z-IETD-FMK 是一种特异性的 caspase 8 抑制剂。- 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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Bcl-2 inhibitor
Sabutoclax（BI-97C1）是一种泛Bcl-2抑制剂，包括对Bcl-xL、Bcl-2、Mcl-1和Bfl-1的抑制，其IC50分别为0.31 μM、0.32 μM、0.20 μM和0.62 μM。- Christopher D. Graham, .et al. , Oncotarget, 2017, Jan 31; 8(5): 8670-8678 PMID: 28055968
