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Search results for: Caspase 3 Inhibitor Z DEVD FMK

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#32457417   2020/05/26 To Up

Gasdermin E-derived caspase-3 inhibitors effectively protect mice from acute hepatic failure.

Programmed cell death (PCD), including apoptosis, apoptotic necrosis, and pyroptosis, is involved in various organ dysfunction syndromes. Recent studies have revealed that a substrate of caspase-3, gasdermin E (GSDME), functions as an effector for pyroptosis; however, few inhibitors have been reported to prevent pyroptosis mediated by GSDME. Here, we developed a class of GSDME-derived inhibitors containing the core structure of DMPD or DMLD. Ac-DMPD-CMK and Ac-DMLD-CMK could directly bind to the catalytic domains of caspase-3 and specifically inhibit caspase-3 activity, exhibiting a lower IC than that of Z-DEVD-FMK. Functionally, Ac-DMPD/DMLD-CMK substantially inhibited both GSDME and PARP cleavage by caspase-3, preventing apoptotic and pyroptotic events in hepatocytes and macrophages. Furthermore, in a mouse model of bile duct ligation that mimics intrahepatic cholestasis-related acute hepatic failure, Ac-DMPD/DMLD-CMK significantly alleviated liver injury. Together, this study not only identified two specific inhibitors of caspase-3 for investigating PCD but also, more importantly, shed light on novel lead compounds for treating liver failure and organ dysfunctions caused by PCD.
Wan-Feng Xu, Quan Zhang, Chu-Jie Ding, Hui-Yong Sun, Yuan Che, Hai Huang, Yun Wang, Jia-Wei Wu, Hai-Ping Hao, Li-Juan Cao

2384 related Products with: Gasdermin E-derived caspase-3 inhibitors effectively protect mice from acute hepatic failure.

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#32104028   2020/02/10 To Up

Caspase-3 Promotes Diabetic Kidney Disease Through Gasdermin E-Mediated Progression to Secondary Necrosis During Apoptosis.

Apoptosis has been repeatedly linked with diabetic kidney disease (DKD), which is a programmed cell death mediated by effector caspases-3, 6 and 7, targeting >600 substrates. However, the pathophysiologic correlations of this process remain obscure. As a putative tumor suppressor, gasdermin E (GSDME) was recently reported to be cleaved by caspase-3 to produce a GSDME-N fragment which targets the plasma membrane to switch apoptosis to secondary necrosis. However, it remains elusive whether GSDME is involved in the regulation of DKD.
Si Wen, Zhao-Hua Wang, Cong-Xiao Zhang, Ying Yang, Qiu-Ling Fan

1954 related Products with: Caspase-3 Promotes Diabetic Kidney Disease Through Gasdermin E-Mediated Progression to Secondary Necrosis During Apoptosis.

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#31947862   2020/01/03 To Up

Isoflavones Isolated from the Seeds of Induced Apoptotic Cell Death in Human Ovarian Cancer Cells.

The seeds of are used in fishing, pesticides, and folk medicine in Ethiopia. Here, the anti-cancer effects of isoflavones isolated from were evaluated in human ovarian cancer cells. We found that isoflavone ferrugone and 6,7-dimethoxy-3',4'-methylenedioxy-8-(3,3-dimethylallyl)isoflavone (DMI) had potent cytotoxic effects on human ovarian cancer cell A2780 and SKOV3. Ferrugone and DMI treatment increased the sub-G1 cell population in a dose-dependent manner in A2780 cells. The cytotoxic activity of ferrugone and DMI was associated with the induction of apoptosis, as shown by an increase in annexin V-positive cells. Z-VAD-fmk, a broad-spectrum caspase inhibitor, and z-DEVD-fmk, a caspase-3 inhibitor, significantly reversed both the ferrugone and DMI-induced apoptosis, suggesting that cell death stimulated by the isoflavones is mediated by caspase-3-dependent apoptosis. Additionally, ferrugone-induced apoptosis was found to be caspase-8-dependent, while DMI-induced apoptosis was caspase-9-dependent. Notably, DMI, but not ferrugone, increased the intracellular levels of reactive oxygen species (ROS), and antioxidant N-acetyl-L-cysteine (NAC) attenuated the pro-apoptotic activity of DMI. These data suggest that DMI induced apoptotic cell death through the intrinsic pathway via ROS production, while ferrugone stimulated the extrinsic pathway in human ovarian cancer cells.
Yi-Yue Wang, Jun Hyeok Kwak, Kyung-Tae Lee, Tsegaye Deyou, Young Pyo Jang, Jung-Hye Choi

2358 related Products with: Isoflavones Isolated from the Seeds of Induced Apoptotic Cell Death in Human Ovarian Cancer Cells.

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#31698777   2019/11/06 To Up

Farnesiferol C Induces Apoptosis in Chronic Myelogenous Leukemia Cells as an Imatinib Sensitizer via Caspase Activation and HDAC (Histone Deacetylase) Inactivation.

Herein the underlying apoptotic mechanism of Farnesiferol C (FC) derived from was elucidated in chronic myelogenous leukemia (CML) K562 and KBM5 cells. FC showed significant cytotoxicity in K562 and KBM5 cells, more so than in U937 and UL-60 acute myeloid leukemia (AML) cells. Cleaved PARP and caspase 9/3 attenuated the expression of Bcl2 and induced G1 arrest in K562 and KBM5 cells. Also, FC effectively abrogated the expression of cell cycle related proteins, such as: Cyclin D1, Cyclin E, Cyclin B1 in K562, and KBM5 cells, but caspase 3 inhibitor Z-DEVD-FMK rescued the cleavages of caspase 3 and PARP induced by FC in K562 cells. Of note, FC decreased histone deacetylase 1 (HDAC1) and HDAC2, and enhanced histone H3 acetylation K18 (Ac-H3K18) in K562 and KBM5 cells. Furthermore, combination of FC and Imatinib enhanced the apoptotic effect of Imatinib as a potent Imatinib sensitizer in K562 cells. Overall, our findings provide scientific evidence that inactivation of HDAC and caspase activation mediate FC induced apoptosis in CML cells.
Ji Hoon Jung, Ji Eon Park, Deok Yong Sim, Eunji Im, Woon Yi Park, Duckgue Lee, Bum-Sang Shim, Sung-Hoon Kim

2500 related Products with: Farnesiferol C Induces Apoptosis in Chronic Myelogenous Leukemia Cells as an Imatinib Sensitizer via Caspase Activation and HDAC (Histone Deacetylase) Inactivation.

100 assays200 Tests2 ml100 assays1 kit100ug1 kit 50 UG96 assays4 Membranes/Box100 assays

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#31612876   // To Up

Sensitive detection of caspase-3 enzymatic activities and inhibitor screening by mass spectrometry with dual maleimide labelling quantitation.

There is a great need to develop sensitive and specific methods for quantitative analysis of caspase-3 activities in cell apoptosis. Herein, we report a new method for sensitive detection of caspase-3 enzyme activities and inhibitor screening based on dual maleimide (DuMal) labeling quantitation and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). Evaluation of caspase-3 activities is performed using MS analysis of the enzymatic product of the peptide probe, which fuses a caspase-3 cleavable peptide segment (DEVD) and a quantifiable "ID tag" (a peptide segment of FRGLRGFKC labeled by maleimide). The DuMal labeling technique features non-isotopic tagging, rapid reactions, and reproducible quantitation. We have achieved quantitative analysis of the enzyme activities with a limit of detection (LOD) and limit of quantitation (LOQ) of caspase-3 down to 0.11 nM and 0.29 nM respectively and a proof-of-concept demonstration of its inhibitor screening. Our method has further been tested for caspase-3 activities in a Parkinson's disease cellular model, suggesting a useful tool for protease activity research.
Fuzhong Ouyang, Tianrong Yu, Chao Gu, Guanghui Wang, Rui Shi, Rui Lv, Enhui Wu, Chongqing Ma, Ruochen Guo, Jing Li, Anna Zaczek, Jian Liu

1762 related Products with: Sensitive detection of caspase-3 enzymatic activities and inhibitor screening by mass spectrometry with dual maleimide labelling quantitation.

100 assays100 assays100 assays100 assays100 assays100 assays100 assays100 assays100 assays100 assays5 mg96 tests

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#31029906   2019/01/28 To Up

Reactive oxygen species mediate the chemopreventive effects of syringin in breast cancer cells.

Syringin (Syr), a phenylpropanoid glycoside extracted from Eleutherococcus senticosus, possesses various biological properties, including anticancer activities. However, the cytotoxicity effects of Syr on breast cancer have not yet been elucidated.
Chien-Hsing Lee, Chiung-Wei Huang, Po-Chih Chang, Jun-Ping Shiau, In-Pin Lin, Mei-Ying Lin, Chih-Cheng Lai, Chung-Yi Chen

1472 related Products with: Reactive oxygen species mediate the chemopreventive effects of syringin in breast cancer cells.



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#30904799   2019/03/21 To Up

Combined Administration of Poly-ADP-Ribose Polymerase-1 and Caspase-3 Inhibitors Alleviates Neuronal Apoptosis After Spinal Cord Injury in Rats.

Neuronal apoptosis plays a pivotal role in spinal cord injury (SCI)-induced secondary cellular events. Caspase-dependent and -independent pathways are involved in neuronal apoptosis. Caspase-3 is the final effector of caspase-dependent apoptosis, whereas poly-ADP-ribose polymerase-1 (PARP-1) and apoptosis-inducing factor (AIF) are key executors of caspase-independent apoptosis. However, it remains unclear whether simultaneous inhibition of the 2 apoptosis pathways will be more beneficial for neuronal survival. Therefore, this study investigated the ability of coadministration of the PARP-1 inhibitor 3-aminobenzamide (3-AB) and caspase-3 inhibitor z-DEVD-fmk to attenuate apoptosis in a rat SCI model.
Wei Zhao, Hongxing Li, Yun Hou, Yinchuan Jin, Lianshuang Zhang

2004 related Products with: Combined Administration of Poly-ADP-Ribose Polymerase-1 and Caspase-3 Inhibitors Alleviates Neuronal Apoptosis After Spinal Cord Injury in Rats.

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