カスパーゼ
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S2228 | Belnacasan (VX-765) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7023 | Z-VAD-FMK | <1 mg/mL | 93 mg/mL | <1 mg/mL |
| S7313 | Z-LEHD-FMK | 44 mg/mL | 100 mg/mL | 100 mg/mL |
| S7314 | Z-IETD-FMK | <1 mg/mL | 91 mg/mL | <1 mg/mL |
| S7312 | Z-DEVD-FMK | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7311 | Q-VD-OPh | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8102 | Z-VAD-FMK (Caspase Inhibitor VI) | <1 mg/mL | 90 mg/mL | 90 mg/mL |
| S7775 | Emricasan | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7901 | Ac-DEVD-CHO | 100 mg/mL | -1 mg/mL | -1 mg/mL |
| S2738 | PAC-1 | <1 mg/mL | 78 mg/mL | 16 mg/mL |
| S2927 | Apoptosis Activator 2 | <1 mg/mL | 61 mg/mL | <1 mg/mL |
| S7326 | Tasisulam | <1 mg/mL | 83 mg/mL | 83 mg/mL |
| s9097 | Alisol B Acetate | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S2448 | Gambogic Acid | <1 mg/mL | 100 mg/mL | 100 mg/mL |
亜型選択性的な製品
Caspase製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. 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 is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
(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.
|
|
| S7313新 |
Z-LEHD-FMKZ-LEHD-FMK is a specific, irreversible Caspase-9 inhibitor. |
||
| S7314 |
Z-IETD-FMKZ-IETD-FMK is a specific Caspase-8 inhibitor. |
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 is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and 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 is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. |
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-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
-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.
|
|
| S7775 |
EmricasanEmricasan is a potent irreversible pan-caspase inhibitor. |
||
| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. |
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.
|
|
| S2738 |
PAC-1PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3. |
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 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. |
||
| S7326 |
TasisulamTasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
||
| s9097新 |
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 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. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2228 |
Belnacasan (VX-765)Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. 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 is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells. |
(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.
|
|
| S7313新 |
Z-LEHD-FMKZ-LEHD-FMK is a specific, irreversible Caspase-9 inhibitor. |
||
| S7314 |
Z-IETD-FMKZ-IETD-FMK is a specific Caspase-8 inhibitor. |
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 is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and 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 is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. |
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-FMK (Caspase Inhibitor VI)Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor. |
-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.
|
|
| S7775 |
EmricasanEmricasan is a potent irreversible pan-caspase inhibitor. |
||
| S7901 |
Ac-DEVD-CHOAc-DEVD-CHO is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2. |
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.
|
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2738 |
PAC-1PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3. |
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 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells. |
||
| S7326 |
TasisulamTasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3. |
2016, 29(6):281-290 |
|
| s9097新 |
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 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. |
