目录号
产品名
应用
产品描述
文献引用
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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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Caspase activator
PAC-1 是一种激活 procaspase-3 的化合物，能够在癌细胞中诱导凋亡，其半数有效浓度（EC50）为 2.08 微摩尔。- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Apoptosis Activator
Apoptosis Activator 2 强烈诱导 caspase-3 激活、PARP 切割和 DNA 碎片化，这导致细胞的破坏（依赖 Apaf-1）, 其半抑制浓度（IC50）约为 4 微摩尔，对 HMEC、PREC 或 MCF-10A 细胞无效。 -
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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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。 -
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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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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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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Caspase-3 Inhibitor
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
- 25-羟基胆固醇是一种从饮食中的胆固醇衍生的侧链取代型氧固醇，它通过抑制固醇调节元件结合蛋白（SREBPs）的切割，从而抑制各种细胞类型中内源性胆固醇的合成。
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Caspase-9 Inhibitor
Z-LEHD-FMK 是一种合成肽，可以不可逆地抑制 caspase-9 及相关 caspase 活性。- 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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osteoblast differentiation inducer
Asperosaponin VI，一种来自川牛膝（Dipsacus asper wall）的皂苷成分，通过 BMP-2/p38 和 ERK1/2 通路诱导成骨细胞分化。Asperosaponin VI 抑制缺氧诱导的心肌细胞凋亡，通过增加 Bcl-2/Bax 比例和减少活性 caspase-3 表达，以及增强 p-Akt 和 p-CREB。 -
Caspase inhibitor
Q-VD-OPH 是一种选择性的、能渗透大脑和细胞的、高效且不可逆的抑制剂，主要针对 caspase-3（IC50=25nm）、caspase-1（IC50=50nM）、caspase-8（IC50=100nM）和 caspase-9（IC50=430nM）。- 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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Caspase-3/7 Inhibitor
Caspase-3/7 Inhibitor I 是一种强效的、细胞渗透性的、特异性的可逆抑制剂，专门针对 caspase-3（Ki = 60 nM）和 caspase-7（Ki = 170 nM）。 -
Caspase-3 inhibitor
AZ 10417808，选择性非肽类caspase-3抑制剂（Ki = 247 nM）；对caspases 1、2、6、7和8的选择性超过40倍（Ki > 10 uM）。 -
Caspase-3 inhibitor
Ivachtin 是一种强效的、细胞渗透性的、可逆的、非竞争性的 Caspase-3 抑制剂（IC50 = 23 nM）。- Yosefzon Y, .et al. , Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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Fluorogenic caspase substrate
Ac-LEHD-AFC 是一种荧光底物，适用于 caspase-4、caspase-5 和 caspase-9。 -
Caspase-1 inhibitor
Z-YVAD-FMK 是一种强效的、可渗透细胞并且不可逆的 caspase-1 抑制剂。- 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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insecticidal and anticancer
Destruxin B，从昆虫病原真菌Metarhizium anisopliae中分离出来，是一种具有杀虫和抗癌活性的环肽。Destruxin B通过依赖Bcl-2家族的线粒体途径诱导人类非小细胞肺癌细胞的凋亡。 - Lycopodine，一种从石松孢子中提取的药理学上重要的生物活性成分，通过调节5-脂氧合酶和去极化线粒体膜电位，触发难治性前列腺癌细胞的凋亡，而不调节p53活性。Lycopodine通过激活caspase-3诱导凋亡，从而抑制HeLa细胞的增殖。
- Guggulsterone 是从树种 Commiphora wightii 的树脂中提取的植物甾体。Guggulsterone 通过下调抗凋亡基因产品（IAP1、xIAP、Bfl-1/A1、Bcl-2、cFLIP 和 survivin）、调节细胞周期蛋白（cyclin D1 和 c-Myc）、激活 caspases 和 JNK、抑制 Akt，抑制多种肿瘤细胞的生长并诱导凋亡。
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anticancer agent
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP), a renowned medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein. 5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration-dependent manner. -
Caspase-1 substrate
Ac-YVAD-pNA 是一个特定的 Caspase-1 底物。Ac-YVAD-pNA 可用于检测 Caspase-1 活性。Caspase-1 是炎症过程的关键介质。
