Caspase
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
Caspase产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。 |
(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
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| S7023 |
Z-VAD-FMKZ-VAD-FMK是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。 |
(A) LAN5 cells were untreated (top panels) or treated with 50 µM of the caspase inhibitor Z-VAD-FMK (bottom panels). Cells were co-treated with nothing (No Rx), 1 µM GSK-J4, or 1 µM venetoclax for 48 hours and assayed for apoptosis by flow cytometry.
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| S7313New |
Z-LEHD-FMKZ-LEHD-FMK是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。 |
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| S7314 |
Z-IETD-FMKZ-IETD-FMK是一种特异性Caspase-8抑制剂。 |
The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
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| S7312 |
Z-DEVD-FMKZ-DEVD-FMK是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。 |
Immunoblotting analysis was performed for the active-caspase-3 and cleavage of MCL-1 in MM.1S cells treated with z-DEVD-fmk (20 μM, 1 h) and following GSK126 (25 μM, 24 h).
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| S7311 |
Q-VD-OphQ-VD-OPh是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。 |
UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
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| S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI)是一类不可逆的泛caspase抑制剂。 |
-FMK-S810201Z0220161121.gif)
-FMK-S810201Z0220161121.gif)
Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
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| S7775 |
EmricasanEmricasan是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。 |
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| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。 |
Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. *P<0.05 vs. the control group, **P<0.01 vs. the control group.
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| S2738 |
PAC-1PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。 |
The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
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| S2927 |
Apoptosis Activator 2Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。 |
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| S7326 |
TasisulamTasisulam是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3 |
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| s9097New |
Alisol B AcetateAlisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
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| S2448 |
Gambogic AcidGambogic Acid激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
-Mucosal-Immunol-20150929.gif)
-FMK-Med-Oncol-20161108.gif)
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765)是一种有效的选择性caspase-1抑制剂，无细胞试验中Ki为0.8 nM。Phase 2。 |
(D and E) Caspase-1 inhibitors (Ac-YVAD-CMK and VX765) were added during the induction of trastuzumab-dependent BT-474 (red) or rituximab-dependent Raji cell phagocytosis (green). MFI of PD-L1 (D) and IDO (E) in macrophages are as indicated.
|
|
| S7023 |
Z-VAD-FMKZ-VAD-FMK是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。 |
(A) LAN5 cells were untreated (top panels) or treated with 50 µM of the caspase inhibitor Z-VAD-FMK (bottom panels). Cells were co-treated with nothing (No Rx), 1 µM GSK-J4, or 1 µM venetoclax for 48 hours and assayed for apoptosis by flow cytometry.
|
|
| S7313New |
Z-LEHD-FMKZ-LEHD-FMK是一种具有细胞透性、不可逆的Caspase-9抑制剂，有助于细胞生存。 |
||
| S7314 |
Z-IETD-FMKZ-IETD-FMK是一种特异性Caspase-8抑制剂。 |
The caspase-8 inhibitors do not rescue NB4 cells from TPEN-triggered apoptosis. NB4 cells were pre-treated with 50 μM Z-ITED-FMK or 100 μM Ac-IETD-CHO for 1 h, and then treated with 5 μM TPEN for 24 h. (A) Cell morphology was observed and recorded using an optical microscope. The scale bar represents 20 μm. A partiallty enlarged view was shown in the lower left corner of every picture. (B) Apoptosis rate was measured with Annexin V/PI dual staining by flow cytometry.
|
|
| S7312 |
Z-DEVD-FMKZ-DEVD-FMK是一种特异性，不可逆的Caspase-3抑制剂，也能有效抑制caspase-6， caspase-7， caspase-8和caspase-10。 |
Immunoblotting analysis was performed for the active-caspase-3 and cleavage of MCL-1 in MM.1S cells treated with z-DEVD-fmk (20 μM, 1 h) and following GSK126 (25 μM, 24 h).
|
|
| S7311 |
Q-VD-OphQ-VD-OPh是一种有效的pan-caspase抑制剂，作用于caspases 1， 3， 8和9，IC50范围在25到400 nM之间，有效抑制与细胞凋亡相关的末端caspase激活，底物裂解，及DNA梯状条带形成。 |
UA and Q-VD-Oph attenuated TNF-α-induced unclear translocation of NF-κB (C) and P-STAT3(S727) (D) in BEAS-2B cells.
|
|
| S8102 |
Z-VAD(OH)-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI)是一类不可逆的泛caspase抑制剂。 |
Effect on the RAS of CFZ, z-VAD-fmk, or CFZ+z-VAD-fmk treatments administered 5 or 12 days after C26 inoculation and control groups. Serum levels of a renin and b ANGII. c The mRNA expression of ATF2. d Western blot analysis of ATF2 and pATF2. e pATF2-to-ATF2 ratio. Significant differences were detected between most of the groups, with the exceptionsof (A and B) CP and UT (D) and ZP and ZT (#); and (C and E) CP and UP (*), CT and UT (#), and HC, ZP, ZT and CC (&). ZP:z-VAD-fmk.
|
|
| S7775 |
EmricasanEmricasan是有效的、不可逆的泛半胱天冬酶（pan-caspase）抑制剂。 |
||
| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO是Group II caspases的有效抑制剂，对caspase-3和caspase-7的Ki值分别为0.2 nM和1.6 nM。对caspase-2制剂效果弱，Ki值为1.7 μM。 |
Microwave (MW) hyperthermia triggers cell death through caspase-3-mediated apoptosis. H460, PC-9 and H1975 cells were treated with or without Ac-DEVD-CHO for 3 h prior to MW hyperthermia (43°C for 90 min), then allowed to recover at 37°C until 24 h. (A) Cell viability was determined by CCK-8 assay. Data are expressed as the means ± SEM of 3 independent experiments. *P<0.05 vs. the control group, **P<0.01 vs. the control group.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2738 |
PAC-1PAC-1是一种有效的procaspase-3（酶原-3）激活剂，EC50为0.22 μM，是第一个已知的直接激活酶原e-3为caspase-3的小分子。 |
2015, 10.4172/0974-8369.1000259 |
The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.
|
| S2927 |
Apoptosis Activator 2Apoptosis Activator 2强诱导caspase-3激活， PARP分裂， DNA断裂，导致细胞破坏(Apaf-1依赖性的)，IC50约为4 μM，抑制HMEC， PREC和MCF-10A细胞活性。 |
||
| S7326 |
TasisulamTasisulam是一种抗肿瘤剂，是通过内源途径导致细胞凋亡的诱导物。 Phase 3 |
2016, 29(6):281-290 |
|
| s9097New |
Alisol B AcetateAlisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways. |
||
| S2448 |
Gambogic AcidGambogic Acid激活caspases，EC50为0.78 - 1.64 μM，且完全抑制Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 和 Mcl-1，IC50分别为1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM 和 0.79 μM。 |
