目录号
产品名
应用
产品描述
文献引用
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Pan Caspase 抑制剂
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 抑制剂
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）。 -
p53 抑制剂
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 抑制剂
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 抑制剂
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 抑制剂
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。 -
eIF2α dephosphorylation 抑制剂
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 抑制剂
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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XIAP/cIAP1 拮抗剂
Birinapant，也被称为 TL32711，是一种合成的小分子和肽类模拟物，模仿线粒体来源的凋亡激活因子（SMAC）并抑制IAP（凋亡抑制蛋白）家族蛋白，具有潜在的抗肿瘤活性。- Antonella Antignani, .et al. , FASEB J, 2023, Dec;37(12):e23292 PMID: 37971407
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NF-κB 抑制剂
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 抑制剂
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 抑制剂
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 抑制剂
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
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Bax activator
BAM 7 通过与 BAX 的触发位点结合，其 EC50 约为 3.3 微摩尔，该数据通过使用 FITC-BIM SAHB 和 BAX 的竞争性荧光偏振（FP）测定得出。- Takino JI, .et al. , Sci Rep, 2019, Nov 13;9(1):16717 PMID: 31723205
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Cdc42 GTPase 抑制剂
CASIN 是一种新型且强效的 Cdc42 抑制剂。- Yongru Xu, .et al. , Int J Mol Sci, 2017, Mar; 18(3): 586 PMID: 28282856
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Apoptosis inducer
LY573636 是一种强效的抗肿瘤剂，能够在体外和体内抑制多种人类实体瘤的生长并诱导凋亡。LY573636 诱导的凋亡是通过针对线粒体的机制发生的。- Yingzheng Xu, .et al. , JCI Insight, 2024, Jun 13:e174746 PMID: 38869957
- Ting TC, .et al. , Cell Rep, 2019, Nov 5;29(6):1499-1510.e6 PMID: 31693891
- Ting Han, .et al. , Science, 2017, Apr 28;356(6336). pii: eaal3755 PMID: 28302793
- Trifloxystrobin（CGA 279202）是一种杀菌剂，对于大型溞幼体和胚胎，其48小时处理后的EC50分别为23.0微克/升和1.7微克/升。
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HO-1 抑制剂
锌原卟啉（Zn(II)-protoporphyrin IX）是一种竞争性的血红素氧合酶-1（HO-1）抑制剂，显著减弱了苯三酚（PG）对抗 H2O2 的保护效果。- Beixian Zhou, .et al. , MedComm, 2024, Apr 12;5(4):e531 PMID: 38617435
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Caspase-3 抑制剂
Z-DEVD-FMK 是一种特异性的、不可逆的 Caspase-3 抑制剂。- 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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PERK 抑制剂
GSK2656157 是一种与 ATP 竞争的 PERK 酶活性抑制剂，其 IC(50) 为 0.9 nmol/L。它对 PERK 具有高度选择性，其 IC(50) 值在针对 300 种激酶的测试中均 >100 nmol/L。- 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
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pan Bcl-2 抑制剂
AT101，即棉酚乙酸的 R-(-) 对映体，与 Bcl-2、Bcl-xL 和 Mcl-1 结合，其 Ki 分别为 0.32 微米、0.48 微米和 0.18 微米；不抑制 BIR3 域和 BID。 -
Bcl-2 抑制剂
Bcl-2 抑制剂包含两种互变异构体的混合物。这种强效的、细胞渗透性 Bcl-2 抑制剂 能够在体外与 Bak BH3 肽竞争结合到 Bcl-2 和 Bcl-XL（分别的 IC50 为 10 uM 和 7 uM）。- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
